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A9950 Aniracetam ≥98% Aniracetam is a piracetam analog and has low bioavailability due to rapid excretion. It enhances the cognitive thinking and is effective for treatment of sleep and behavioral disorders. Aniracetam is prescribed for anxiety and also enhances learning and memory in situations with induced damage of the brain.
Cognition enhancer (nootropic) that potentiates AMPA receptor mediated ion conductance and potentiates metabotropic glutamate receptor activity.
human ... GRM1(2911), GRM2(2912), GRM3(2913), GRM4(2914), GRM5(2915), GRM6(2916), GRM7(2917), GRM8(2918)
rat ... Gria1(50592)
B7283 Benserazide hydrochloride ≥98% (HPLC), solid Benserazide can block HK2 enzymatic activity in vitro. It is used along with levodopa to treat Parkinson′s disease.
Inhibitor of L-aromatic amino acid decarboxylase.
human ... DDC(1644)
B7273 Bezafibrate ≥98%, solid Bezafibrate has the ability to repress HCV assembly and secretion. It is used to treat dyslipidemia.
The peroxisome proliferator-activated receptor (PPAR) is a member of the steroid nuclear receptor superfamily. Bezafibrate is a peroxisome proliferator-activated receptor agonist for PPARα, PPARδ, and PPARγ. Lipoprotein lipase (LPL) activator.
PPARgamma agonists, including Bezafibrate, have beneficial effects in the suppression of the inflammatory response during RSV infection and therefore might have clinical efficacy in the course of severe RSV-infection.
human ... HBA2(3040), PPARA(5465), PPARD(5467), PPARG(5468)
mouse ... Ppara(19013), Ppard(19015), Pparg(19016)
B8685 BM 15766 sulfate ≥98% (HPLC), powder Dehydrocholesterol reductase inhibitor. Inhibits 7-dehydrocholesterol reductase, which catalyzes the last step of cholesterol synthesis.
 
B6434 Bretazenil ≥96% (HPLC), solid Bretazenil is a benzodiazepine partial agonist.
 
B3023 Bumetanide ≥98% Inhibitor of Na+/K+/Cl- cotransporter.
human ... SLC12A1(6557)
C6239 Cinalukast ~98% (HPLC) Specific CysLT1 leukotriene receptor antagonist.
human ... CYSLTR1(10800)
C1277 Clonazepam powder Anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)
rat ... Tspo(24230)
D0899 Diazepam Diazepam is a benzodiazepine anxiolytic agent. It serves as a prototype ligand for the GABAA receptor benzodiazepine modulatory site.
Diazepam is often used as a sedative. Its metabolism involves cytochrome P450 (CYP) 2C19 and 3A4. Diazepam has immediate action upon administration.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)
rat ... Gabra1(29705), Gabra2(29706)
D7571 Dimaprit dihydrochloride ≥98% (NMR) The histamine H2 receptor influences various cardiovascular responses, including vasodilation and cardiac rhythm, regulates gastric acid secretion, and also plays a role in the immune system by inhibiting antibody production, T cell proliferation and cytokine production. Histamine receptors are members of the GPCR family, and H2 mediates cell signaling via internalization and interaction with the GTPase dynamin.
 
F6300 Flumazenil >99% (HPLC), solid Highly specific benzodiazepine receptor antagonist.
human ... BZRAP1(9256), GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)
rat ... Gabra2(29706), Gabrg1(140674)
F5021 Flunisolide ≥97%    
F9261 Flunitrazepam Hypnotic; anxiolytic; ligand for the GABAA receptor benzodiazepine modulatory site.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)
rat ... Gabra2(29706)
G2536 Ganciclovir ≥99% (HPLC), powder Ganciclovir is a pro-drug nucleoside analog that is activated by phosphorylation. It is useful in the study of gene therapy in cancer research.
Upon expression of a viral suicide gene encoding thymidine kinase, the non-toxic pro-drug is converted to a phosphorylated active analog and is incorporated into the DNA of replicating eukaryotic cells, causing death of the malignant dividing cell. The cell cycle is irreversibly arrested at the G2-M checkpoint. Gap junction involvement in the ganciclovir bystander effect has been studied. Ganciclovir has been used to study loss of telomeres and to evaluate sensitivity of viruses to antiviral treatments.
 
G0639 Glybenclamide ≥99% (HPLC) Glybenclamide is a sulfonylurea class of antidiabetic drug used in the treatment of type 2 diabetes mellitus. It has benzamide moiety and stimulates pancreatic β cells to produce insulin resulting in a hypoglycemic effect. It selectively blocks ATP-sensitive K+ channels in the brain with high-affinity binding sites and elicits cardiovascular effects. It may be a potential therapeutic for thromboembolic disorders due to its in vivo antiplatelet functionality. Glybenclamide traverses to the ischemic brain and provides neuroprotection especially during the early stages of stroke.
Selectively blocks ATP-sensitive K+ channels; high affinity binding sites found in brain, pancreatic β cells, and cardiovascular system.
human ... ABCC8(6833), KCNH2(3757), KCNJ1(3758), KCNJ11(3767)
rat ... Kcnj1(24521)
G3796 Granisetron hydrochloride ≥98% (HPLC), solid Granisetron hydrochloride helps to block nausea/emesis and abdominal pain in irritable bowel syndrome, that is stimulated by chemotherapy.
Granisetron hydrochloride is a serotonin 5-HT3 receptor antagonist and antiemetic.
 
I5784 Ibandronate sodium salt ≥97% (NMR), solid Ibandronate is a nitrogen-containing bisphosphonate (N-BP). It potentially inhibits mevalonate pathway in osteoclasts. Thus, ibandronate is effectively used to treat osteoporosis and other bone-related diseases.
Ibandronate sodium inhibits farnesyl diphosphate synthase (IC50 = 20 nM). Ibandronate sodium is also a bone resorption inhibitor. It has been investigated for in vitro anti-tumor effects, such as apoptosis induction, inhibitor of cell growth, inhibition of invasive behavior, and inhibition of angiogenesis and for its in vivo role in various cancers including breast and prostate cancers.
human ... FDPS(2224)
I2409 Ilmofosine ≥97% (NMR), semisolid (waxy) Protein Kinase C (PKC) inhibitor; an ether lipid derivative of lysophosphatidylcholine has antineoplastic activity in vitro and in vivo. IC50 = 560 nM. Competitive at the regulatory site of PKC. Ilmofosine is active against a variety of explanted human non-small cell lung, breast, colorectal, ovarian, renal cell cancer, and melanoma tumors in vitro at concentrations of 1-30 μg/mL.
 
SML0042 Lazabemide hydrate ≥97% (HPLC) Lazabemide is a selective and reversible monoamine oxidase B (MAO-B) inhibitor and Anti-Parkinson. Also it inhibits monoamine uptake at high concentrations (IC50 values are 86, 123 and > 500 μM for noradrenalin, serotonin and dopamine uptake respectively).
Lazabemide is effective in treatment of Alzheimer′s disease and in combination with nicotine replacement therapy aids in smoking cessation.
 
L121 Levallorphan tartrate salt ≥98% (HPLC), powder Partial agonist (antagonist) at μ and δ opioid receptors.
human ... OPRD1(4985), OPRM1(4988)
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.
 
M5441 Mibefradil dihydrochloride hydrate ≥98% (HPLC), powder Mibefradil is a tetralol derivative and nondihydropyridine calcium channel blocker. It blocks long-type (L-type) calcium channels. It blocks mildly the Purkinje-type (P-type) calcium channels in Purkinje neurons.
Ro 40-5967 is a T-type Ca2+ channel blocker; antihypertensive.
 
UC429 Midazolam hydrochloride solid Sedative/hypnotic; ligand for the GABAA receptor benzodiazepine modulatory site; CYP3A4 substrate.
human ... ABCB1(5243), CYP3A4(1576), GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)
mouse ... Abcb1a(18671), Abcb1b(18669)
rat ... Gabbr1(81657), Gabra1(29705)
M2419 Midazolam maleate salt Sedative/Hypnotic; ligand for the GABAA receptor benzodiazepine modulatory site; CYP3A4 substrate.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)
M3071 Moclobemide ≥98% (HPLC), solid Moclobemide acts as a substrate for cytochrome P450 2C19 (CYP2C19). It also behaves as an inhibitor of cytochrome P450 2D6 (CYP2D6), cytochrome P450 1A2 (CYP1A2 and CYP2C19. Moclobemide is also involved in the increased expression of B-cell lymphoma 2 (BcL-2). It also causes neural stem cell (NSC) differentiation into serotoninergic neuron by extracellular‐regulated kinase (ERK) pathway.
Moclobemide is a reversible monoamine oxidase A inhibitor (MAOI); antidepressant. Elimination half-life in humans = 1 -3 hrs; absolute oral bioavailability. Unlike other MAO inhibitors, does not significantly increase blood pressure in humans upon combination with tyramine.
 
N0287 NNC 55-0396 hydrate ≥98% (HPLC) NNC-55-0396 is a T-type calcium channel antagonists. It is the structural analog of mibefradil. NNC-55-0396 has the ability to block cell proliferation and stimulate cell apoptosis in leukemia cell lines.
Selective T-type calcium channel inhibitor
 
N6287 Nutlin-3 ≥98% (HPLC), powder Nutlin-3 is a Mdm2 (mouse double minute 2) antagonist, p53 pathway activator, and apoptosis inducer.
Nutlin-3, an antagonist of a human homolog of murine double minute 2 (HDM2). It has the ability to inhibit the HDM2-directed degradation of p53. Nutlin-3 can also enhance the transcriptional activities of p73.
 
O4139 Orlistat ≥98%, solid Orlistat impairs intestinal fat absorption and is effective in weight management. It is regarded as a safe drug for treating obesity. It delays the progression of type 2 diabetes mellitus especially in obese and improves glycemic parameters. Long term usage of orlistat results in improved weight reduction and it may not contribute in colorectal carcinogenesis.
Orlistat, used in obesity research, is a pancreatic lipase inhibitor that acts locally in the gastrointestinal tract to inhibit lipase.
human ... LIPF(8513), PNLIP(5406)
R7150 Ro 25-6981 hydrochloride hydrate ≥98% (HPLC), powder Potent and selective antagonist of NMDA glutamate receptors containing the NR2B subunit.
human ... GRIN2B(2904)
R8782 Ro4368554 ≥98% (HPLC) Ro4368554 is a 5-HT6 receptor antagonist. RO4368554 acts selectively at 5-HT6 receptors where it binds with a greater than 100-fold selectivity over other monoamine receptor subtypes (-log M pKi = 9.4 at 5-HT6 and 7.1 at 5-HT2A).
 
R109 Ro 15-4513 solid Benzodiazepine receptor partial inverse agonist; anxiogenic; ethanol antagonist.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA5(2558), GABRA6(2559)
rat ... Gabrg1(140674)
R140 Ro 04-6790 dihydrochloride solid Selective 5-HT6 serotonin receptor antagonist.
human ... HTR6(3362)
R0529 Ro 90-7501 ≥98% (HPLC) Inhibitor of Aß42 fibril formation
 
R8900 Ro 8-4304 solid NR2B-selective, noncompetitive NMDA glutamate receptor antagonist
human ... GRIN2B(2904)
R0279 Ro 23-9358 ≥97% (HPLC), solid Diacylglycerol lipase inhibitor. Target for anti-obesity drugs.
 
R2533 RS-127445 hydrochloride ≥98% (HPLC), powder RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi=9.5) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
 
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.
 
T2952 Tetrabenazine ≥98% (HPLC), solid Tetrabenazine is a reversible type 2 vesicular monoamine transporter (VMAT) inhibitor. It depletes dopamine stores.
 
SML0150 Tolcapone ≥98% (HPLC) Inhibition of catechol-O-methyltransferase by tolcapone increases the half-life and bioavailabilty of levodopa. It therefore is an effective adjunctive therapy in patients with Parkinson′s disease with motor response fluctuations.
Tolcapone is an orally active catechol-O-methyltransferase (COMT) inhibitor. It inhibits both central and peripheral COMT. Tolcapone crosses the blood-brain barrier, and has been used for L-DOPA adjunct therapy in the treatment of Parkinson′s Disease.
human ... COMT(1312)
T3202 Torsemide ≥98% (HPLC), solid Torsemide functions in the thick ascending limb of the loop of Henle and enhances the excretion of sodium, chloride and water from the luminal side of the cells. Furthermore, torsemide can treat oedematous conditions that are associated with diseases such as liver cirrhosis, kidney disorders and chronic congestive heart failure2.
Torsemide is a loop diuretic of the pyridine-sulfonylurea class with antialdosteronergic properties and inhibitor of the Na+/K+/2Cl- carrier system.
human ... SLC12A1(6557)
SML0191 Valganciclovir hydrochloride hydrate ≥98% (HPLC) Valganciclovir hydrochloride hydrate is an antiviral used to treat cytomegalovirus infection. It is the prodrug of ganciclovir, a synthetic analog of 2′-deoxy-guanosine which is phosphorylated to a dGTP analog that competitively inhibits the incorporation of dGTP by viral DNA polymerase.
Valganciclovir is a valine ester of Ganciclovir, used to treat cytomegalovirus retinitis in HIV-infected patients. It is rapidly metabolized to ganciclovir by hydrolysis before entering the systemic circulation resulting in improved absorption of the drug.