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A2736 Anastrozole ≥98% (HPLC) Anastrozole, which contains a triazole functional group, reversibly binds to the cytochrome P-450 component of aromatase. Binding interferes with the catalytic properties of aromatase, which results in inhibition of estrogen synthesis.
The aromatase enzyme converts adrenal androgens to estrogen; this enzymatic activity is the primary source of estrogen production in postmenopausal women. One treatment for estrogen receptor-positive breast cancer in postmenopausal women is through inhibition of aromatase. Anastrozole is a nonsteroidal, benzyl-triazole derivative that inhibits aromatase through competitive inhibition and is used to treat estrogen receptor-positive breast cancer. This compound is considered a third-generation, Type II aromatase inhibitor because it is more selective and less effective (if at all) on other steroidal hormones than first and second generation inhibitors.
A3230 AR-A014418 ≥98% (HPLC), solid Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that has been implicated in pathological conditions such as diabetes and Alzheimer′s disease. GSK3 inhibitor, AR-A014418, inhibits GSK3 (IC50 = 104 nM), in an ATP-competitive manner (Ki = 38 nM). AR-A014418 does not significantly inhibit cdk2 or cdk5 (IC50 > 100 μM) or 26 other kinases, demonstrating high specificity for GSK3.
SML0178 ARL-17477 dihydrochloride hydrate ≥98% (HPLC) ARL-17477 is an nNOS specific inhibitor. The IC50 against rat nNOS is 35 nM and it has 100-fold selectivity over endothelial and inducible isoforms. ARL-17477 penetrates the brain, and reduces infarct size and reduces cerebral blood flow in several different rodent models of ischemic brain injury.
A7655 Atenolol ≥98% (TLC), powder Selective β1-adrenoceptor antagonist; antihypertensive; antianginal; antiarrhythmic.
human ... ADRB1(153)
rat ... Adrb1(24925)
A7231   AZ11645373 ≥98% (HPLC), solid AZ11645373 is a selective and potent human P2X7 purinoceptor antagonist. KB values range from 5-20 nM for human P2X7 receptor inhibition. It is 500-fold less effective ats an inhibitor of rat P2X7 receptor responses.
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.
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.
human ... AR(367)
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.
human ... IFNG(3458), IL5(3567), NR3C1(2908)
rat ... Nr3c1(24413)
C1240 Chlormethiazole hydrochloride ≥98% (HPLC), powder Chlormethiazole serves as an anticonvulsant. It is useful in treating alcohol addiction and eclampsia. Chlormethiazole is also useful in treating convulsive status epilepticus. Long term administration of chlormethiazole leads to addiction to the drug.
GABAA agonist; glycine receptor modulator.
D6068 N-[4-[(6,7-Dimethoxy-4-quinazolinyl)amino]phenyl]benzamide hydrochloride ≥98% (HPLC), solid Aurora Kinase Inhibitor
E7906 Esomeprazole magnesium hydrate ≥98% (HPLC) Esomeprazole magnesium dihydrate is a leading proton pump inhibitor.
F9677 Felodipine solid L-type calcium channel blocker
human ... CACNA1C(775), CACNA1D(776), CACNA1F(778), CACNA1S(779), CACNA2D1(781), NR3C2(4306)
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.
human ... ESR1(2099), ESR2(2100)
G8293 Galanin (2-11) porcine, rat ≥97% (HPLC), lyophilized powder Studies in mice show that injection of galanin (2-11) has anticonvulsant activity in seizure affected animals with an intact DR (dorsal root)–hippocampal serotonergic profile, and has no effect in animals with absent 5-HT (hydroxytryptamine) profile.
rat ... Gal(29141)
G4919 Goserelin acetate ≥99% (HPLC), white powder Goserelin acetate peptide results in significant inhibition of gonadotropin release and suppresses steroidogenesis in ovaries and testis. Thus, it leads to a reduction of testosterone to castration levels and estrogen to postmenopausal levels. Therefore, this peptide is used for reducing testosterone levels in patients with locally advanced prostate cancer.
Goserelin is a synthetic analog of LHRH (leutinizing hormone releasing hormone). Goserelin is a LHRH agonist It is used in prostate cancer and breast cancer therapies and also in the treatment of endometriosis.
human ... GNRH1(2796), GNRHR(2798)
mouse ... GNRH1(14714), GNRHR(14715)
rat ... GNRH1(25194), GNRHR(81668)
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.
human ... ESR1(2099), ESR2(2100), ESRRG(2104), IL6(3569)
rat ... Ar(24208), Esr1(24890), Esr2(25149)
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.
human ... ESR1(2099), ESR2(2100), ESRRG(2104), IL6(3569)
rat ... Ar(24208), Esr1(24890), Esr2(25149)
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.
M9020 Mecamylamine hydrochloride Noncompetitive nicotinic acetylcholine receptor antagonist; preferentially blocks nicotinic receptors at autonomic ganglia; crosses blood-brain barrier.
human ... CHRNA1(1134), CHRNA10(57053), CHRNA2(1135), CHRNA3(1136), CHRNA4(1137), CHRNA5(1138), CHRNA6(8973), CHRNA7(1139), CHRNA9(55584), CHRNB1(1140), CHRNB2(1141), CHRNB3(1142), CHRNB4(1143)
M2574 Meropenem trihydrate ≥98% (HPLC) Meropenem trihydrate is an ultra-broad spectrum beta-lactam antibiotic active against both Gram-positive and Gram-negative bacteria.
O104 Omeprazole solid Omeprazole binds covalently to proton pump (H+, K+-ATPase) and inhibits gastric secretion. It is useful in ameliorating the effects of peptic oesophagitis, duodenal and gastric ulcer. Omeprazole is preferred over antagonists of histamine H2-receptor and ranitidine for its higher efficiency. It is also useful in treating Zollinger-Ellison syndrome.
human ... ABCB1(5243), ATP4A(495), ATP4B(496), CYP1A2(1544)
P9547 Prilocaine hydrochloride ≥98% (TLC) Used for local nerve block and for spinal anesthesia; pharmacological properties are similar to those of lidocaine.
human ... SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
G7048 Proguanil hydrochloride ≥95% (HPLC) Chlorguanide (proguanil) is combined with atovaquone for malaria prophylaxis. The two compounds act synergistically to inhibit the plasmodial dihydrofolate reductase (DHFR) and interrupt the electron transport chain. Mutations in DHFR account for the development of resistant strains.
P0689 (R)-(+)-Propranolol hydrochloride ≥98% (TLC) Less active enantiomer of propranolol.
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
human ... ADRB1(153), ADRB2(154), ADRB3(155), HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355)
P0884 (±)-Propranolol hydrochloride ≥99% (TLC), powder Propranolol hydrochloride is a β-adrenoceptor antagonist. Its action at β2 receptor results in bronchoconstriction. Due to its lipophilic nature, propranolol can penetrate to the central nervous system and has a negative effect. It serves as a 5-HT1/5-HT2 serotonin receptor antagonist. Propranolol hydrochloride is useful as an antihypertensive drug, cardiac depressant and also in the treatment of angina pectoris. It decreases the effect of stress and exercise on heart by reducing the rate of contraction and conduction of impulse. It is known to competitively block the action of catecholamines.
human ... ADRB1(153), ADRB2(154), ADRB3(155), HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358)
Q3638 Quetiapine hemifumarate salt ≥98% (HPLC) Quetiapine hemifumarate is an atypical antipsychotic, a combined serotonin (5HT2) and dopamine (D2) receptor antagonist.
Quetiapine promotes oligodendrogenesis in vitro. It is used in treating depressive disorders.
human ... DRD2(1813), HTR2A(3356), HTR2C(3358)
R9156 Raltitrexed ≥98% (HPLC), solid Raltitrexed is a folate-based inhibitor of thymidylate synthase (TS) that is rapidly and extensively metabolized to its more potent polyglutamate derivatives. By inhibiting the formation of precursor pyrimidine nucleotides, raltitrexed prevents the formation of DNA and RNA, which are required for the growth and survival of both normal cells and cancer cells.
R0758 Ritodrine hydrochloride β2-adrenoceptor agonist; relaxes uterine muscle contraction.
human ... ADRB2(154)
R0283 Ropivacaine hydrochloride monohydrate ≥98% (HPLC) Local anaesthetic with less cardiotoxicity than bupivacaine; causes reversible blockade of impulse propagation along nerve fibres by preventing the inward movement of sodium ions through the cell membrane of the nerve fibers.
Ropivacaine less lipophilic as compared with bupivacaine. It is metabolized in the liver by the enzyme cytochrome P4501A2. Ropivacaine elicits less central nervous system (CNS) toxicity and is used as a local anaesthetic during postoperative and labour pain.
T5648 Tamoxifen ≥99% Protein kinase C inhibitor. Induces apoptosis in human malignant glioma cell lines. Tamoxifen and its metabolite 4-hydroxytamoxifen are selective estrogen response modifiers (SERMs) that act as estrogen antagonists in mammary gland. Blocks estradiol-stimulated VEGF production in breast tumor cells.
human ... CYP1A2(1544), EBP(10682), ESR1(2099), ESR2(2100), ESRRA(2101)
rat ... Ar(24208), Esr1(24890)
T9262 Tamoxifen citrate salt ≥99% Protein kinase C inhibitor. Induces apoptosis in human malignant glioma cell lines. Tamoxifen and its metabolite 4-hydroxytamoxifen are selective estrogen response modifiers (SERMs) that act as estrogen antagonists in mammary gland. Blocks estradiol-stimulated VEGF production in breast tumor cells.
human ... ESR1(2099), PRKCA(5578), PRKCB(5579), PRKCD(5580), PRKCE(5581), PRKCG(5582), PRKCH(5583), PRKCI(5584)
T0202 Tocainide hydrochloride ≥98% (HPLC), solid Tocainide hydrochloride is a primary amine analog of lidocaine (lignocaine), used for the treatment of tinnitus. It blocks the sodium channels in the pain-producing foci in the nerve membranes and renders an analgesic effect in trigeminal neuralgia.
Tocainide hydrochloride is a sodium channel blocker; Class IB antiarrhythmic.
human ... SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
Z4152 Zafirlukast ≥98% (HPLC) Zafirlukast is a potent subtype specific cysteinyl leukotriene type 1 receptor (CysLT1) antagonist; antiasthmatic. Zafirlukast has over 1000-fold selectivity for CysLT1, one of two receptors for cysteinyl leukotrienes LTC4, LTD4, and LTE4, which are important mediators of human bronchial asthma.
Zafirlukast plays a key role in alleviating mucus and airway constriction in asthma based inflammatory response. It regulates pancreatic β cells for the secretion of insulin and this functionality is interlinked to the calcium based phosphorylation of the Ca2+/calmodulin-dependent protein kinase II (CaMKII) and protein kinase B (AKT). Zafirlukast has inhibitory potential on ATP-binding cassette (ABC) transporters and reverses the multidrug resistance function of ATP-binding cassette super-family G member 2 (ABCG2). Zafirlukast inhibits mycobacterial nucleoid-associated protein Lsr2 and halts the growth of Mycobacteria.
human ... CYSLTR1(10800)
Z3777 ZD7288 hydrate ≥98% (HPLC) Selective blocker of cation channel Ih; If blocker and sino-atrial node function modulator, blocks hyperpolarization-activated and cyclic nucleotide-gated (HCN) channels.
ZD7288 can block hippocampal synaptic plasticity.
Z101 Zimelidine dihydrochloride solid Serotonin transport blocker; antidepressant.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)