Fluorination Ready Pharma-Developed Compounds

A select offering of Pharma-Developed bioactive small molecules, both approved therapeutics/drug candidates and tool compounds, is tailored for potential use in Late Stage Functionalization. The compounds selected can be modified to include fluorine, which, despite appearing sparingly in naturally-occurring compounds, is found in fully 25% of FDA approved drugs.

Solutions to incorporate fluorine into your Lead compound are explored further in our Fluorination Application Guide.

Specifically, phenolic and alkyl carbinols can be converted directly to fluorine using PhenoFluor, a late-stage deoxyfluorination reagent.

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I2760 (−)-Isoproterenol (+)-bitartrate salt powder β-Adrenoceptor agonist; increases cytosolic cAMP.
Isoproterenol functions as an ovine pulmonary vein dilator.
P134 (−)-Pentazocine ≥98% (HPLC)  
M0267 (±)-Methadone hydrochloride powder, ≥98% μ opioid receptor agonist that desensitizes both the μ opioid receptor and the δ opioid receptor on chronic exposure; narcotic analgesic, characterized by a gradual onset of action and prolonged, milder withdrawal; may also block L-type calcium channels independently of its effects on opioid receptors.
S0278 (±)-Sotalol hydrochloride ≥98% (TLC), powder Potent β-adrenoceptor antagonist; class III antiarrhythmic; prolongs the action potential and increases the refractory period.
Sotalol has a potential to block non-cardioselective β-adrenergic receptors. It acts as an anti-arrhythmic agent and is used as a therapeutic for equine arrhythmias. In addition, sotalol also has an ability to stop atrial fibrillation recurrence.
P127 (+)-Pentazocine solid σ receptor agonist; active enantiomer of pentazocine.
P6126 (R)-(−)-Phenylephrine hydrochloride powder α1-adrenoceptor agonist.
P0689 (R)-(+)-Propranolol hydrochloride ≥98% (TLC) Less active enantiomer of propranolol.
B6309 (R)-Butaprost ≥98% (HPLC) (R)-Butaprost is a selective EP2 prostanoid receptor agonist.
Butaprost comprises hydroxy-cyclopentanone ring and ω-chain. It aids protection in events of glutamate based N-methyl-D-aspartate receptor toxicity. Butaprost inhibits conjunctival fibrosis and lowers the intraocular pressure in post glaucoma filtration surgery. It also promotes wound healing by reducing the subconjunctival scarring Tenon′s fibroblasts. Butaprost plays a protective role in pulmonary fibrosis and aids protection against the aggregated amyloid β (Aβ) peptides in Alzheimer′s disease.
P8688 (S)-(−)-Propranolol hydrochloride ≥98% (TLC), powder (S)-(−)-Propranolol hydrochloride is biologically active enantiomer. It acts as β1 receptor antagonist in thalamocortical neurons. (S)-(−)-Propranolol hydrochloride elicits its inhibitory function on the β1 adrenoceptor in trigeminovascular pain pathway and serves as a preventive medicine in migraine.
Active β-adrenoceptor blocking enantiomer, as measured by inhibition of isoprenaline-induced tachycardia; Propranolol is also non-specific 5-HT1A, 5-HT1B and 5-HT1C serotonin receptor antagonist. The stereoselective association of mianserin and propranolol with the 5HT1A, 5HT1B and 5HT1C sites may prove useful in the characterization of these sites
H7904 (Z)-4-Hydroxytamoxifen ≥98% Z isomer 4-Hydroxytamoxifen (4-HT) is the active metabolite of tamoxifen which binds estrogen receptors (ER) and estrogen-related receptors (ERR) with estrogenic and anti-estrogenic effects. It is a cell permeable, selective estrogen receptor modulator (SERM). In Cas9 variants engineered with ligand-dependent inteins 4-Hydroxytamoxifen was used control Cas9 function, which reduced off target effects in CRISPR-mediated gene editing.
H6278 4-Hydroxytamoxifen ≥70% Z isomer (remainder primarily E-isomer) Metabolite of the chemotherapeutic drug tamoxifen, exhibiting more potent estrogen agonist/antagonist activity than the parent drug. Also active as intra-membranous inhibitor of lipid peroxidation.
A3656 5-Aza-2′-deoxycytidine ≥97% 5′-Azadeoxycytidine causes DNA demethylation or hemi-demethylation. DNA demethylation can regulate gene expression by "opening" the chromatin structure detectable as increased nuclease sensitivity. This remodeling of chromatin structure allows transcription factors to bind to the promoter regions, assembly of the transcription complex, and gene expression. Decitabine is an epigenetic modifier that inhibits DNA methyltransferase activity which results in DNA demethylation (hypomethylation) and gene activation by remodeling "opening" chromatin. Genes are synergistically reactivated when demethylation is combined with histone hyperacetylation.
A2385 5-Azacytidine ≥98% (HPLC) 5-Azacytidine (Aza-CR) acts as a potential chemotherapeutic regimen for acute myelogenous leukemia. This drug has an ability to selectively increase γ-globin synthesis. Therefore, 5-azacytidine is used in treating severe β-thalassemia. Aza-CR acts as a potential bacteriostatic, antitumor and mutagenic agent. In addition, it also exhibits various biological activity such as, immunosuppressive, antimitotic, radioprotective and virostatic effects.
A potent growth inhibitor and cytotoxic agent; inhibits DNA methyltransferase, an important regulatory mechanism of gene expression, gene activation and silencing.
Causes DNA demethylation or hemi-demethylation, creating openings that allow transcription factors to bind to DNA and reactivate tumor suppressor genes.
A2846 A-134974 dihydrochloride hydrate ≥98% (HPLC), solid A-134974 is a novel and selective adenosine kinase (AK) inhibitor with IC50 = 60 pM. Systemic A-134974 (i.p.) dose dependently reduced hyperalgesia (ED50= 1 μmol/kg) and at higher doses, reduced locomotor activity (ED50 = 16 μmol/kg). Administration of A-134974 intrathecally (i.t.) was more potent (ED50= 6 nmol) at producing antihyperalgesia than delivering the compound by intracerebralventricular (ED50 = 100 nmol, i.c.v.) or intraplantar (ED50 >300 nmol) routes. In contrast, i.c.v. administration of A-134974 was more effective in reducing locomotor activity than i.t. administration (ED50 values were 1 and >100 nmol, respectively). Increasing the pretreatment time for i.t.-delivered A-134974 caused a greater reduction in locomotor activity (ED50= 10 nmol). This was due to diffusion of A-134974 (i.t.) to supraspinal sites. These data demonstrate that the novel AK inhibitor A-134974 potently reduces thermal hyperalgesia primarily through interactions with spinal sites, whereas its ability to depress locomotor activity is predominantly mediated by supraspinal sites.
A3477 AH 11110 >98% (HPLC), solid α1B-adrenoceptor ligand
A9102 AH13205 ≥98% (HPLC), oil AH13205 is a selective, low potency agonist for the EP2 receptor. AH13205 has been shown to compete with Prostaglandin E2 (PGE2) for binding, resulting in the displacement of PGE2 binding.
SML0074 Acenocoumarol ≥98% (HPLC) Acenocoumarol is a warfarin analog, an anticoagulant that inhibits Vitamin K epoxide reductase. This results in depletion of the reduced form of vitamin K (vitamin KH2), limiting the gamma-carboxylation and subsequent activation of the vitamin K-dependent coagulation factors II, VII, IX, and X and anticoagulant proteins C and S, resulting in decreased prothrombin levels and the amount of thrombin generated.
Acenocoumarol is effective against thromboembolic disorders.
A7655 Atenolol ≥98% (TLC), powder Selective β1-adrenoceptor antagonist; antihypertensive; antianginal; antiarrhythmic.
A3480 Atosiban ≥98% (HPLC) Atosiban efficiently prevent preterm uterine contractions without any major cardiovascular, pulmonary or central nervous system side effects. It has potential to treat preterm labour.
Atosiban is a peptide oxytocin receptor antagonist.
A0132 Atropine ≥99% (TLC), powder Atropine is used to treat myopia and ocular axial elongation in Asian children. Small dosage of atropine is used to slow down the heart rate.
Competitive nonselective antagonist at central and peripheral muscarinic acetylcholine receptors.
PZ0007 Azithromycin dihydrate ≥98% (HPLC) Azithromycin dihydrate is a macrolide antibiotic, azalide subclass. It binds to the 50S subunit of the 70S bacterial ribosomes and inhibits RNA-dependent protein synthesis in bacterial cells. Azithromycin also has anti-immunomodulatory/anti-inflammatory properties, which make it useful in treating cystic fibrosis.
Azithromycin is a non-β-lactam antibody, effective against infections associated with respiratory tract, skin, tissues and genital chlamydia. It also acts against Plasmodium falciparum and P. vivax, which are multidrug resistance species that transmit malaria. Azithromycin targets the ribosome and prevents protein synthesis. It is soluble in lipids and metabolizes in liver by undergoing demethylation.
B8684 Bambuterol hydrochloride >98% (HPLC), powder β-adrenoceptor agonist; bronchodilator; anti-asthmatic; terbutaline prodrug
Bambuterol hydrochloride is used for prophylaxis and also to treat chronic bronchitis and chronic asthma in pediatrics.
B9680 Bay u9773 ≥98% (HPLC), oil Subtype-selective cysteinyl-leukotriene (Cys-Lt) antagonist.
B0385 Beclomethasone ≥99% Beclomethasone is an anti-inflammatory glucocorticoid.
It helps to decrease airway hyperresponsiveness. It also helps to regulate symptoms of asthma.
B0515 Betamethasone 17-valerate Betamethasone 17-valerate is a synthetic glucocorticoid. It exhibitstherapeutic effects against various allergic and inflammatory skin diseases. Betamethasone 17-valerate also possesses anti-inflammatory properties.
B5683 Betaxolol hydrochloride >98% (HPLC) Betaxolol hydrochloride has the ability to block calcium channels. Betaxolol is a selective β1 adrenoreceptor antagonist. It has neuroprotective effects on retinal neurons.
B9061 Bicalutamide (CDX) ≥98% (HPLC), powder Bicalutamide (CDX) is a non-steriodal Androgen Receptor (AR) antagonist and a pure antiandrogen. It acts via balancing histone acetylation/deacetylation and recruitment of coregulators. Bicalutamide (CDX) abolishes androgen-mediated expression. For example, MMP13 upregulation in prostate cancer, PLZF (promyelocytic leukemia zinc finger protein), and GADD45γ (growth arrest and DNA damage inducible, gamma). Bicalutamide (CDX) is inhibited by non-genomic, transcription-independent stimulation of PI3K/AKT phosphorylation by androgens.
B2185 Bisoprolol hemifumarate salt ≥98% (HPLC), solid Bisoprolol hemifumarate is useful in oral formulations due to its high bioavailability. It also shows long elimination half-life.
Cardioselective β1-adrenoceptor antagonist.
B7777 Budesonide ≥99% Budesonide is a second generation glucocorticoid with low systemic absorption. It is used as an anti-inflammatory agent in the treatment of asthma, rhinitis, and inflammatory bowel disease. It inhibits the expression of chemokine mRNA and production of eotaxin and RANTES protein in primary human bronchial epithelial cells. Budesonide is currently in clinical trials for the prevention of lung cancer. It shows inhibitory effects on benzo[a]pyrene-induced carcinogenesis of the lung in mice.
B1935 Butorphan S(+)-mandelate ≥98% (HPLC), solid κ/μ opioid receptor agonist.
B9156 Butorphanol (+)-tartrate salt ≥99% κ/μ opioid receptor agonist.
C5976 CL 316,243 hydrate ≥98% (HPLC), powder CL 316,243 is a β3 adrenoceptor agonist; anti-obesity agent.
β Adrenoceptor is expressed in a number of tissues such as heart, adipose tissue, colon and other tissues. It is associated with many different biological functions. β Adrenoceptor fills in as an objective for treating type 2 diabetes, heart failure, cachexia, obesity, metabolic disorder, issues related with bladder, colon and malignant tumor growth. Depression and anxiety can also be treated via β adrenoceptor. CL 316,243 is known to have antidiabetic action via β adrenoceptor. It is a potent stimulator of lipolysis. It also activates β3- adrenoceptors on neurons in hypothalamic areas that are important in the central regulation of appetite.
SML0053 CP-101,606 ≥98% (HPLC) CP-101,606 (Traxoprodil) plays a role in inhibiting glutamate-induced death in rats. It may exhibit therapeutic effects against human ischemia and neurodegenerative disorders. Traxoprodil is metabolized by cytochrome P450 (CYP) 2D6.
Traxoprodil (CP-101,606) is a potent noncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptors, selective for the NR2B subunit. It has been shown to be neuroprotective in animal models of brain injury and stroke.
C1112 CP-55940 >98% (HPLC), powder CP-55940 is a nonclassical cannabinoids (NCCs), which lack the tetrahydropyran ring. CP-55940, a derivative of CP-47,497 is enantioselective. Due to its amphipathic nature, CP-55940 tethers in biological membrane making it favourable for the cannabinoid receptor interaction. CP-55940 belongs to the cyclohexylphenol category and modulates the brain lipidome leading to dysregulation especially during adolescence. It inhibits capsaicin-evoked sensitization of nociceptive and spinal dorsal horn neurons.
CP-55940 is a selective cannabinoid receptor agonist.
PZ0130 CP-64434 hydrate ≥98% (HPLC) CP-064434 is an antibiotic; anti-proliferative HDAC inhibitor.
C2247 CPPHA ≥98% (HPLC) CPPHA is a selective positive allosteric modulator of mGluR5 receptor. It has no agonist activity alone, but reduces threshold response and shifts dose-response curves to glutamate, quisqualate, and DHPG by 4- to 7-fold to the left in recombinant CHO cells expressing human or rat mGluR5.
SML0005 Cerivastatin sodium salt hydrate ≥98% (HPLC) Accumulated macrophages in atherosclerotic plaques result in plaque rupture and thrombus formation. Cerivastatin suppresses the growth of macrophages and decreases the expression of matrix metalloproteinases and tissue factor molecules, thus reduces acute coronary events.
Cerivastatin sodium is an HMG-CoA reductase inhibitor. HMG-CoA is a key enzyme in the production of cholesterol.
C7495 Clofarabine ≥98% (HPLC) Clofarabine is a purine nucleoside antimetabolite. Clofarabine is toxic to nondividing lymphocytes and monocytes.
Clofarabine is a second-generation nucleoside analog, used in cancer treatments. Clofarabine is metabolized to 5′-triphosphate and is known to block DNA synthesis. The human equilibrative nucleoside transporters (hENT1 and hENT2) and human concentrative nucleoside transporter (hCNT2 and hCNT3) mediates clofarabine transport into the cell. It also serves as a substrate for mitochondrial deoxyguanosine kinase. Clofarabine is an inhibitor of ribonucleotide reductase. It resists the phosphorolytic cleavage catalyzed by purine nucleoside phosphorylase of bacterias. Clofarabine also withstands deamination by adenosine deaminase.
D2069 Desvenlafaxine hydrochloride ≥98% (HPLC), powder Desvenlafaxine hydrochloride is a dual SERT/NET reuptake inhibitor. It is a major active metabolite of venlafaxine (#542); brain penetrant; Ki = 40 nM and 122 nM for hSERT and hNET, respectively (weak binding at the hDAT). Inhibition of [3H]5-HT or [3H]NE uptake for the hSERT or hNET produced IC50 values of 47 and 531 nM.
Desvenlafaxine hydrochloride is a psychoactive drug. Incidence of this drug in environmental samples might induce in vitro gene expression associated with neurological disorders.
D1756 Dexamethasone ≥98% (HPLC), powder Dexamethasone is known to be effective against relapsed multiple myeloma. It is found to decrease inflammation associated with cerebrospinal fluid and central nervous system (CNS) complications, such as hearing loss.
Glucocorticoid anti-inflammatory agent. Regulates T cell survival, growth, and differentiation. Inhibits the induction of nitric oxide synthase.
E2031 Eliprodil ≥98% (HPLC), powder NR2B selective NMDA glutamate receptor antagonist which appears to target the "polyamine site" on the NMDA receptor, setting it apart from other NR2B receptor antagonists. Possesses neuroprotective effects in models of ischemia, but prolongs the QT interval in patients; currently under investigation for acute and chronic pain.
E8031 Esmolol hydrochloride ≥98% (HPLC), solid Esmolol hydrochloride is a ultrashort-acting β1 adrenoceptor antagonist (β1 receptor occupancy = 84.7%).
E3638 Estazolam Hypnotic; ligand for the GABAA receptor benzodiazepine modulatory site.
E2661 Estropipate ≥98% (HPLC), powder Estropipate is the piperazine salt of the estrogen receptor agonist estrone-3-sulfate and a potent, specific inhibitor of the organic anion transporting polypeptide 1B1 (OATP1B1, IC50 = 60 nM).
E5406 Ethopropazine hydrochloride ≥98% (HPLC), powder Ethoproprazine hydrochloride is an inhibitor of butyrylcholinesterase; antiparkinsonian. It reduces extrapyramidal motor effects, characteristic of Parkinson′s disease; also alleviates thermal hyperalgesia in rats.
E1383 Etoposide synthetic, 98.0-105.0%, powder Etoposide is an antitumor agent that complexes with topoisomerase II and DNA to enhance double-strand and single-strand cleavage of DNA and reversibly inhibit religation. Blocks the cell cycle in in S-phase and G2-phase of the cell cycle; induces apoptosis in normal and tumor cell lines; inhibits synthesis of the oncoprotein Mdm2 and induces apoptosis in tumor lines that overexpress Mdm2.
Etoposide is used in treating advanced testicular cancer, Kaposi′s sarcoma, non-small cell lung cancer (NSCLC), SCLC (small cell lung cancer) and lymphoma.
PZ0006 Exemestane ≥98% (HPLC) Exemestane is a steroidal antiestrogen and irreversible aromatase inhibitor. Exemestane acts as a false substrate for the aromatase enzyme. Exemestane also prevents the conversion of androgens to estrogens and is used to treat estrogen-dependent breast cancer.
F8182 Faropenem sodium hydrate ≥98% (HPLC) Faropenem sodium is an ultra-broad spectrum, β-lactamase resistant, β-lactam antibiotic active against both Gram-positive and Gram-negative bacteria.
F1016 Fenoterol hydrobromide β2-adrenoceptor agonist; bronchodilator.
F9427 Fexofenadine hydrochloride >98% (HPLC) Fexofenadine is a non-sedating H1 histamine receptor antagonist.
Fexofenadine is used in treating allergic rhinitis and chronic idiopathic urticaria. It may give relief in bothersome symptom and is a second-generation antihistamines. Fexofenadine provides better relief compared to other antihistamines for nasal congestion. It is the active metabolite of terfenadine and bring down allergen-induced symptoms.
F5021 Flunisolide ≥97%  
SML0038 Fluvastatin sodium hydrate ≥98% (HPLC) Fluvastatin has antifungal activity.
Fluvastatin is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Fluvastatin is antilipemic and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.
I4409 Fulvestrant >98% (HPLC) Fulvestrant (ICI 182,780) is a selective estrogen receptor down-regulator (SERD). Fulvestrant is a high affinity estrogen receptor antagonist. IC50 = 0.29 nM. Fulvestrant is the first "pure" antiestrogen with no agonistic activity both in vitro and in vivo.
Fulvestrant is a 7α-alkylsulphinyl analog of 17β-oestradiol and is structurally different compared to other selective estrogen receptor (ER) modulators (SERMs). It reduces dimerization and nuclear localization of the estrogen receptor (ER). Fulvestrant lowers the level of ER protein in human breast cancer cells. Fulvestrant is preferred for the treatment of women at their menopause having hormone-sensitive advanced breast cancer.
G6173 GSK 4716 ≥98% (HPLC) GSK 4716 is an Estrogen-related receptors ERRβ and ERRγ agonist with minimal activity for ERRα, ERα and ERβ
G6423 Gemcitabine hydrochloride ≥98% (HPLC) Gemcitabine is a widely used antitumor agents in both clinics and research labs. It is an antineoplastic agent and antimetabolite.
I2536 ICI 192605 ≥98% (HPLC) ICI 192605 is a potent thromboxane A2 receptor antagonist. It inhibits platelet aggregation and can reverse the effects of vasoconstrictors such as TXA2 or PGD2. ICI 192605 can reverse vasoconstriction induced by inhibition of NO production by L-NEMA, which leads to an increase in TXA2 release.
I0160 Imipenem monohydrate ≥98% (HPLC) Imipenem is found effective against gram positive and negative aerobes and anaerobes. Imipenem is often combined with cilastatin, to inhibit its metabolism in kidney.
Imipenem monohydrate is a broad spectrum B-lactam antibiotic. It is a member of the carbapenem class of "magic bullet" antibiotics for severe infections.
I5627 Isoprenaline hydrochloride β-adrenoceptor agonist; increases cytosolic cAMP.
L1790 L-685,458 >96% (HPLC), solid L-685,458 is a potent, selective, structurally novel γ-secretase inhibitor; equipotent inhibitor of both Aβ1-42 and Aβ1-40 production.
L-685,458 mimics the transition state in aspartyl protease. It possesses an IC50 of 17nM with respect to inhibition of Aβ synthesis. It is known to block Notch (neurogenic locus notch homolog protein) signaling, which in turn reduces ERK (extracellular signal regulated kinase) phosphorylation by EGF (epidermal growth factor). L-685,458 targets the active site and substrate binding site of the enzyme.
SML0225 LY255582 ≥98% (HPLC) LY255582 inhibits the diet-associated increases in mesolimbic dopamine levels and reduces the consumption of highly-palatable food intake.
LY255582 is a centrally active opioid receptor antagonist (defined as an inverse agonist in 2011 JPET paper) that inhibited weight gain in obese Zucker rats over 30 days. It is more that 5-fold selective for mu opioid receptor compared to kappa opioid receptors and 13-fold selective over delta opioid receptors.
L1011 Labetalol hydrochloride >98% (TLC), powder Competitive β-adrenoceptor antagonist.
L1292 Latanoprost acid ≥98% (HPLC) Potent, selective FP prostanoid receptor agonist, F-series prostaglandin analog. 200 times as potent as isopropyl ester form.
L1167 Latanoprost ≥98% (HPLC) Latanoprost is a potent, selective prostaglandin F2α analog receptor agonist. It is hydrolyzed by esterases into its biologically active form latanoprost acid in the cornea. Latanoprostplays a role in reducing the intraocular pressure (IOP) due to which it has therapeutic effects in treating glaucoma.
L121 Levallorphan tartrate salt ≥98% (HPLC), powder Partial agonist (antagonist) at μ and δ opioid receptors.
L5420 Lumefantrine Lumefantrine is is an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.
SML0115 MDL 11939 ≥98% (HPLC) MDL 11,939 is a potent, selective and orally active 5-HT2 receptor antagonist (ASTAR). Ki values values are in the low nanomolar range for 5-HT2A with over 100-fold selectivity over 5-HT2C receptors and low or no affinity for non-5-HT2 receptors or transporters.
M2319 Mefloquine hydrochloride ≥98% (HPLC), powder Blocker of gap junction channels Cx36 and Cx50.
Mefloquine is broadly used as an antimalarial drug. It inhibits 80S ribosomes of Plasmodium. It has numerous side effects like anxiety, dizziness, tremor, headache, and hearing loss. Mefloquine damages cochlear and vestibular hair cells through apoptosis. It also damages spiral ganglion neurons, degenerates cortical neuron and disrupts neuronal calcium homeostasis.
M2574 Meropenem trihydrate ≥98% (HPLC) Meropenem trihydrate is an ultra-broad spectrum beta-lactam antibiotic active against both Gram-positive and Gram-negative bacteria.
M2537 Mevastatin ≥98% (HPLC), powder or crystals HMG-CoA reductase inhibitor. Cholesterol lowering drug. Inhibits myoblast formation. An antibiotic shown to cause apoptosis, apparently by inhibiting post-translational prenylation of proteins such as Ras. Similarly, mevastatin increases eNOS mRNA and protein levels by blocking the geranylgeranylation of Rho.
M2147 Mevinolin from Aspergillus sp. ≥98% (HPLC) Lovastatin is a cholesterol lowering drug and competitive inhibitor of HMG-CoA reductase, a rate limiting enzyme in cholesterol synthesis. Blocks the production of mevalonate, a critical compound in the production of cholesterol and isoprenoids. This product is a substrate of Pgp and CYP3A. It increases cellular resistance to anticancer agents such as doxorubicin and induces apoptosis in myeloma cells. The roles of Pgp and CYP3A, possible connection between drug resistance, regulation of the mevalonate pathway, and iosprenylation of signaling proteins in these observations remain to be resolved. The product induces apoptosis in numerous cancer cell lines perhaps, in part, by inhibiting the isoprenylation of Rho family GTPases. It causes cell cycle arrest in G1 and G2/M phases.
M9511 Minocycline hydrochloride powder Minocycline is a broad spectrum antibiotic with bacteriostatic function. Minocycline has anti-inflammatory properties. Minocycline inhibits lipopolysaccharide mediated inflammatory cytokine tumour necrosis factor (TNF-α) secretion by macrophages. Minocycline inhibits macrophage proliferation in a dose dependent manner. Minocycline inhibits neuroinflammation in pre-plaque of Alzheimer′s disease-like amyloid pathology through inhibition of key inflammatory enzymes like inducible nitric oxide synthase (iNOS), matrix metalloproteinase 9 (MMP-9) and 5-lipoxygenase. Minocycline inhibits endothelial cell proliferation and angiogenesis. Minocycline exhibits anti-tumor activity in glioma by inhibiting membrane type 1 matrix metalloproteinase (MT1-MMP). Minocycline increases cognition and neuronal differentiation. zMinocycline effectively reduces neuropathic pain by increasing the functions of nociceptin/orphanin FQ.
M4074 Mometasone furoate ≥98% (HPLC) Mometasone furoate is a 17-heterocyclic intranasal corticosteroid. It is effectively used as a first-line daily intranasal therapeutic for allergic rhinitis and nasal polyposis. Mometasone furoate is also used as an adjunct to anti-bacterials for treating acute rhinosinusitis. In addition, it relieves the symptoms of asthma in both adults and adolescents by exhibiting a broad spectrum of anti-inflammatory properties.
Mometasone furoate is an anti-inflammatory glucocorticoid.
M8777 Morphine sulfate salt pentahydrate Narcotic analgesic; prototypic μ opioid receptor agonist; also agonist at κ opioid receptors.
M7694 Mupirocin ≥92% (HPLC), powder Antibiotic; inhibits isoleucyl-tRNA synthetase (IRS).
N7662 Nafarelin acetate salt hydrate ≥95% (HPLC), solid Nafarelin acetate salt hydrate is a gonadotrophin releasing hormone analogue and luteinizing hormone releasing hormone (LH-RH) agonist.
N4396 Nalbuphine hydrochloride hydrate ≥98% (HPLC) Partial agonist for μ and κ opioid receptors.
N165 Naloxone benzoylhydrazone solid Agonist for κ3 opioid receptors; antagonist for ORL1 and μ opioid receptors.
N7758 Naloxone hydrochloride dihydrate ≥98% (TLC and titration), powder Competitive antagonist for μ, κ, δ, and σ opioid receptors; blocks the action of σ-agonists at opioid sites. Naloxone′s antagonistic effect last for about 45 min and thus, requires repeated dosage. It results in critical side effects such as pulmonary edema.
N129 Naloxone methiodide ≥98% (HPLC), solid Naloxone methiodide has low affinity for opioid receptors than naloxone. Administration of naloxone inhibits opioid receptor and opioid-induced respiratory depression.
Quaternary salt of naloxone that, like the parent compound, is a nonselective antagonist at opioid receptors. It does not cross the blood-brain barrier.
N3136 Naltrexone hydrochloride Competitive antagonist for μ, κ, δ, and σ-opioid receptors; has greater oral efficacy and longer duration of action than naloxone.
O3764 Oxcarbazepine ≥98% (HPLC), solid Anticonvulsant, antineuralgic. Inhibits veratrine-induced transmitter release.
PZ0162 PD 0325901 ≥98% (HPLC) PD 0325901 by inhibiting mitogen-activated protein kinases (MAPKs) elicits growth-inhibitory and antiangiogenic effects on glioblastoma and melanoma tumor progression.
PD 0325901 is a potent MKK1 (MEK1) and MKK2 (MEK2) inhibitor. The Ki is 1.1 and 0.79 nM for MEK1 and MEK2, respectively. PD 0325901 was inactive against a panel of 27 other kinases. PD 0325901 inhibited C26 tumor pERK by 75% when dosed at 25 mg/kg in mice.
PZ0111 PD-407824 ≥98% (HPLC) PD-407824 is a Wee1/Chk1 inhibitor.
PZ0131 PF-998425 ≥98% (HPLC) PF-998425 is a novel, nonsteroidal androgen receptor antagonist.
T1912 Paclitaxel from Taxus yannanensis, powder Paclitaxel is a potent anti-neoplastic and anti-mitotic taxane drug, which binds to the N-terminus of β-tubulin and and stabilizes microtubules arresting the cell cycle at the G2/M phase. The microtubule damage induces apoptosis through a JNK-dependent pathway followed by a JNK-independent pathway, perhaps related to the activation of protein kinase A (PKA) or of Raf-1 kinase, resulting in phosphorylation of Bcl-2. A major metabolite via CYP2CB is 6α-hydroxypaclitaxel (6α-OHP).
P0099 Paliperidone ≥98% (HPLC) Paliperidone is an atypical antipsychotic; active metabolite of risperidone.
P7547 Phentolamine hydrochloride ≥98% (TLC), powder α-adrenoceptor antagonist; peripheral vasodilator.
P7561 Phentolamine methanesulfonate salt ≥98% (TLC), powder α-Adrenergic receptor antagonist; peripheral vasodilator.
P0778 Pindolol ≥98% (TLC), powder β1-adrenoceptor antagonist; putative 5-HT1A serotonin receptor agonist; vasodilator.
β1-adrenoceptor antagonist; putative 5-HT1A serotonin receptor agonist; vasodilator. Pindolol is a non-cardioselective beta-adrenergic blocking agent. It possesses intrinsic sympathomimetic activity.
P4498 Pravastatin sodium salt hydrate ≥98% (HPLC), powder Competitive, water-soluble 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor. Inhibits cholesterol synthesis in vivo (Ki ~1 nM).
Pravastatin sodium is a competitive, water-soluble 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor.
P6004 Prednisolone ≥99% Prednisolone is a glucocorticoid with anti-inflammatory and immunosuppressive activity.
P9180 Procaterol hydrochloride β2-adrenoceptor agonist; bronchodilator.
P0130 Progesterone ≥99% Induces maturation and secretory activity of the uterine endothelium; suppresses ovulation. Progesterone is implicated in the etiology of breast cancer.
P4670 Propafenone hydrochloride Blocks hKv1.5 and ATP-sensitive K+ channels; class 1C antiarrhythmic agent that is also an antagonist at β adrenergic receptors.
Q0875 Quinidine sulfate salt dihydrate Class IA antiarrhythmic; potassium channel blocker.
Q3625 Quinidine anhydrous Class IA antiarrhythmic; potassium channel blocker.
Quinidine, an isomer of quinine has potential side effects like proarrhythmia on usage. It prolongs cardiac potential and is sodium channel blocker. It is a potential antagonist for α1-adrenoceptors and contributes to hypotension. It inhibits cytochrome P450 2D6 and improves circulation and brain penetration of dementia drug, dextromethorphan. Quinidine-dextromethorphan combination may be useful in treating pseudobulbar affect (PBA).
Q1250 Quinine hemisulfate salt monohydrate synthetic, ≥90% (HPLC) Potassium channel blocker. Antimalarial, anticholinergic, antihypertensive, and hypoglycemic agent; alkaloid originally isolated from the Cinchona family of South American trees. Inhibits mitochondrial ATP-regulated potassium channel. Used to study the metabolism of biocrystalized heme, hemozoin, in malarial parasites and to study the toxicity of heme (FP)-complexes.
Quinine has analgesic property.
R6152 Ranolazine dihydrochloride ≥98% (HPLC), powder pFOX (partial fatty acid oxidation) inhibitor, a new class of anti-anginal drugs, which inhibit fatty acid beta-oxidation and activates pyruvate dehydrogenase, thereby diverting the heart′s energy source from lipids to glucose, which requires less oxygen and helps maintain myocardiac function at times of ischemia
R0395 Rapamycin from Streptomyces hygroscopicus ≥95% (HPLC), powder A macrocyclic triene antibiotic that binds to and inhibits the molecular target of rapamycin (mTOR). It forms a complex with FKBP12 that binds to and inhibits the molecular target of rapamycin (mTOR). Rapamycin is a potent immunosuppressant and has anticancer activity.
R0758 Ritodrine hydrochloride β2-adrenoceptor agonist; relaxes uterine muscle contraction.
R7150 Ro 25-6981 hydrochloride hydrate ≥98% (HPLC), powder Potent and selective antagonist of NMDA glutamate receptors containing the NR2B subunit.
R8900 Ro 8-4304 solid NR2B-selective, noncompetitive NMDA glutamate receptor antagonist
R9281 Rotigotine hydrochloride ≥98% (HPLC) Rotigotine hydrochloride is a non-ergolinic D3/D2 and D1-dopamine agonist. It is appropriate for transdermal delivery through skin patches, that has the drug in a silicone-based adhesive matrix.
Rotigotine is a dopamine receptor agonist with preference for D3 receptors over D2 and D1. As such, it is an effective anti-Parkinsonian agent. Racemic rotigotine is about 50 times as potent as quinpirole, the gold standard D2 agonist.
P152 S(–)-Pindolol solid β1-adrenoceptor antagonist; putative 5-HT1A serotonin receptor agonist; vasodilator. Active enantiomer of pindolol.
S7076 SB 202190 monohydrochloride hydrate ≥98% (HPLC) SB 202190 binds within the ATP pocket of p38 kinase and inhibits the p38α and β isoforms.
SB 202190 is a highly selective, potent, and cell-permeable inhibitor of p38 MAP kinase.
SB 202190 monohydrochloride hydrate mediates the phosphorylation of serine in the mutant p53 protein and modulates cell adhesion and prevents cell proliferation in breast cancer cell lines.
S7067 SB 202190 ≥98% (HPLC) SB 202190 is a highly selective, potent and cell permeable inhibitor of p38 MAP kinase. SB 202190 binds within the ATP pocket of the active kinase (Kd = 38 nM, as measured in recombinant human p38), and selectively inhibits the p38α and β isoforms.
S3567 SB 415286 ≥98% (HPLC) Glycogen synthase kinase-3 (GSK-3) inhibitor.
SB 415286 is a small molecule inhibitor of GSK-3 in muscle and fat cells. SB 415286 induces activation of glycogen synthase and regulates the transport glucose. SB 415286 reduces the systemic inflammation induced by endotoxic shock in rat model of acute colitis. It increases the axonal growth and promotes the recovery of injured adult CNS neurons. SB 415289 is implicated in inducing chromosome instability when used as therapeutic agents.
SML0015 SR 142948A ≥98% (HPLC) SR 142948A is a non-peptide Neurotensin receptor antagonist
SR 142948A is a potent neurotensin receptor antagonist that affects the expression of c-Fos and has properties of antipsychotic agent. It blocks hypothermia and analgesia induced by neurotensin. It blocks the increase in the concentration of Ca+2 induced by the activation of phospholipase C in CHO cell model.
S8688 SR 59230A ≥98% (HPLC), powder SR 59230A is a β3-adrenoceptor antagonist. It has high affinity for the β3 adrenoceptors occurring in human gut that affect the function of human colonic circular smooth muscle.1 It is reported that SR 59230A inhibits the Kir2.1-2.3 cardiac potassium channels.2
S7201 SR-46349 hemifumarate salt ≥98% (HPLC) ASTAR (Antagonist of Serotonin 5HT2A Receptors).
SR-46349 is an antagonist of 5-HT (2A/2C) receptor and increases the release of dopamine by medial prefrontal cortex in rats.1 It increases the signal transduction induced by 5-HT2 receptor by binding with high affinity.2 SR-46349 inhibits the aggregation of rabbit and human platelets in response to serotonin.3
S8260 Salbutamol β2-adrenoceptor agonist
Salbutamol is a β2 adrenoceptor agonist with short acting bronchodilation and anti-inflammatory effects. It relaxes the airway smooth muscles and inhibits bronchoconstriction induced by adenosine-5′ -monophosphate (AMP).1 Salbutamol is particularly effective in treatment of asthma as it provides immediate relief.2
S5013 Salbutamol hemisulfate salt ≥98% β2-Adrenergic receptor agonist.
Salbutamol is a β2 adrenoceptor agonist with short acting bronchodilation and anti-inflammatory effects. It relaxes the airway smooth muscles and inhibits bronchoconstriction induced by adenosine-5′ -monophosphate (AMP).1 Salbutamol is particularly effective in treatment of asthma as it provides immediate relief.2
Salbutamol is a β2 adrenoceptor agonist with short acting bronchodilation and anti-inflammatory effects. It relaxes the airway smooth muscles and inhibits bronchoconstriction induced by adenosine-5′ -monophosphate (AMP). Salbutamol is particularly effective in treatment of asthma as it provides immediate relief. Salbutamol is one of the most popular short-acting BA (SABA). It is useful in treating the symptoms of EIB (exercise induced bronchospasm).
S8451 Saquinavir mesylate ≥98% (HPLC), powder Saquinavir is an HIV Protease Inhibitor used in antiretroviral therapy. It inhibits both HIV-1 and HIV-2 proteases. Studies have also looked at saquinavir as a possible anti-cancer agent.
S6196 Simvastatin ≥97% (HPLC), solid Simvastatin is a specific inhibitor of HMG-CoA reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, an early step in cholesterol biosynthesis. It is used in the treatment of hypercholesterolemia, as it reduces levels of low-density lipoproteins and triglycerides, and raises high-density lipoprotein levels. Simvastatin is a lactone that is readily hydrolyzed in vivo to the corresponding β-hydroxyacid, and can be activated prior to use with NaOH in EtOH treatment. It is a synthetic analog of lovastatin (Cat. No. M2147).
Simvastatin is a specific inhibitor of HMG-CoA reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, an early step in cholesterol biosynthesis. It is used in the treatment of hypercholesterolemia, as it reduces levels of low-density lipoproteins cholesterol and triglycerides, and raises high-density lipoprotein levels. Simvastatin is a lactone that is readily hydrolyzed in vivo to the corresponding β-hydroxyacid and can be activated prior to use with NaOH in EtOH treatment. It may also have beneficial effects on endothelial function, inflammation, smooth muscle cell function, vascular wall function, hemostasis and LDL oxidation.
PZ0020 Temsirolimus ≥98% (HPLC) Temsirolimus is a specific inhibitor of mammalian target of rapamycin (mTOR) mTOR Complex 1 (mTORC1). Temsirolimus is an antiproliferative and antiangiogenic, the first-in-class mTOR inhibitor approved for the treatment of patients with advanced poor prognosis renal cell carcinoma.
The inhibitory action of temsirolimus is mediated by FKBP-12 (FK506-binding protein 12), a major intracellular protein. It is useful in treating renal-cell carcinoma.
T9652 Terfenadine Non-sedating second generation H1 histamine receptor antagonist. Mainly metabolized by Cyp3A4, 5, 7. Inhibits CYP2C8.
Terfenadine acts a potential anti-histamine and is used in the treatment of allergic rhinitis and chronic urticaria.
PZ0021 Tigecycline hydrate ≥98% (HPLC) Tigecycline is a broad spectrum glycylcycline antibiotic. Tigecycline is bacteriostatic, that inhibits protein synthesis by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline is active against resistant strains of gram-positive and gram-negative bacteria, avoiding the two most common mechanisms of resistance to the tetracycline antimicrobials: tetracycline efflux pump proteins and ribosomal protection proteins.
T6394 Timolol maleate salt ≥98% (TLC), powder Timolol maleate is a class II anti-arrhythmic agent that functions as a non-selective β-adrenoceptor antagonist, a vasodilator and an anti-glaucoma agent. Studies have reported that timolol maleate can be used for the treatment of infantile hemangioma (IH)7.
T7455 Tolvaptan ≥98% (HPLC), powder Tolvaptan (OPC 41061) is a potent, orally active non-peptide vasopressin V2 selective antagonist. IC50 = 3 nM at the rat V2 receptor; 29 times more selective for the V2 than for V1a. Tolvaptan has also been shown to inhibit the development of polycystic kidney disease in several animal models.
T2705 Topotecan hydrochloride hydrate ≥98% (HPLC and enzymatic) Topotecan is a topoisomerase I inhibitor and an apoptosis inducer. It is a potent antineoplastic agent.
T6376 Triamcinolone Triamcinolone is a synthetic glucocorticoid agonist; induces gene expression and apoptosis; inhibits prostaglandin synthesis; impairs tumor necrosis factor (TNF)-α-induced degradation of κB-α; potentiates the differentiation-inducing effects of bone morphogenetic proteins (BMP-2, -4, -6).
W1520 WAY-200070 ≥98% (HPLC) Potent, selective estrogen receptor-beta (ER-β) agonist (IC50 2.3 nM vs 155 nM for ER-α) with anxiolytic-like and antidepressant-like effects.