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B8810 BAY 41-2272 ≥97% (HPLC) BAY 41-2272 is an activator of soluble guanylate cyclase at a novel, NO-independent regulatory site. BAY 41-2272 is the first product that stimulates sGC through a non-NO mechanism. BAY 41-2272 inhibits platelet aggregation and induces vasorelaxation without nitrate tolerance.
B9685 BAY 61-3606 hydrochloride hydrate ≥98% (HPLC), powder BAY 61-3606 helps to prevent the degranulation of freshly isolated basophils. It also prevents B cell receptor (BCR)-mediated signaling.
Spleen tyrosine kinase (Syk) inhibitor; anti-inflammatory. Syk plays a major role in inflammation pathways via receptors for the Fc portion of immunoglobulins, as well as B cell signaling. It is orally active, potent (Ki 7.5 nM), and highly selective for Syk vs other kinases (Lyn, Fyn, Src, Itk, Btk; Ki′s).
B3561 BAY 73-6691 ≥98% (HPLC), powder BAY 73-6691 was characterized in vitro as the first potent and selective inhibitor of phosphodiesterase 9 (PDE9), which is currently under preclinical development for the treatment of Alzheimer′s disease. This compound selectively inhibits human (IC50 = 55 nM) and murine (IC50 = 100 nM) PDE9 activity in vitro and shows only moderate activity against other cyclic nucleotide-specific phosphodiesterases. BAY 73-6691 alone did not significantly increase basal cGMP levels. The PDE9 inhibitor significantly potentiated the cGMP signals generated by sGC activating compounds such as BAY 58-2667 or 5-cyclopropyl-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-4-ylamine (BAY 41-2272) and induced leftward shifts of the corresponding concentration-response curves. The newly generated PDE9 reporter cell line show that BAY 73-6691 is able to efficiently penetrate cells and to inhibit intracellular PDE9 activity.†
B3936 BAY R3401 ≥98% (HPLC), solid BAY R3401 is a glycogen phosphorylase inhibitor. The racemic prodrug, BAY R3401, suppresses hepatic glycogenolysis. BAY W1807, the active metabolite of BAY R3401, inhibits muscle glycogen phosphorylase a and b. It has been investigated that the metabolites of BAY R3401 suppress hepatic glycogenolysis by allosteric inhibition and dephosphorylation of phosphorylase a.
B3686 BAY U6751 hydrate solid, ≥98% (HPLC) BAY W1807, the active metabolite of BAY R3401, inhibits muscle glycogen phosphorylase a and b. In gel-filtered liver extracts, racemic BAY U6751 (containing active BAY W1807) was tested for inhibition of phosphorylase in the glycogenolytic (in which only phosphorylase a is active). In liver extracts, BAY U6751 (0.9-36 μmol/L) inhibited glycogen synthesis by phosphorylase b (notwithstanding the inclusion of AMP), but not by phosphorylase a. Inhibition of phosphorylase-a-catalyzed glycogenolysis was partially relieved by AMP (500 μmol/L). BAY U6751 facilitated phosphorylase-a dephosphorylation. Isolated hepatocytes and perfused livers were tested for BAY R3401-induced changes in phosphorylase-a:b ratios and glycogenolytic output.
B9680 Bay u9773 ≥98% (HPLC), oil Subtype-selective cysteinyl-leukotriene (Cys-Lt) antagonist.
B3563 Bifonazole ≥98% (HPLC) Bifonazole is an imidazole-based anti-fungal agent with broad spectrum activity against many fungi, molds, yeast and some Gram-positive bacteria. Bifonazole inhibits ergosterol biosynthetic protein 28 and Cytochrome P450 2B4.
Bifonazole is used to treat several infections such as onychomycoses, otomycoses, erythrasma, psoriasis, sebopsoriasis, seborrhoeic dermatitis and rosacea. Bifonazole is also used as an important drug to treat melanoma.
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.
SML0020   BX471 ≥98% (HPLC) BX471 blocks CCR1 and downregulates the mRNA expression of ICAM-1, P-selectin and E-selectin. It decreases the inflammatory responses in sepsis, prevents monocyte recruitment in inflammation sites in rheumatoid arthritis patients and inhibits interstitial leukocyte recruitment and fibrosis in mouse model of lupus nephritis.
BX471 is an orally active, CCR-1 specific antagonist. It displaces the endogenous CCR-1 ligands MIP-1a, RANTES and MCP-3 (Ki range 1-5 nM). BX471 inhibits CCR-1 effects in leukocytes, including calcium mobilization and migration.
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.
C3025 (±)-Chlorpheniramine maleate salt ≥99% (perchloric acid titration) Chlorpheniramine maleate (CPM) can prevent rhinitis and urticaria. It is used to cure several allergic conditions. This antihistamine is used in small-animal veterinary practices.
H1 Histamine receptor antagonist.
human ... HRH1(3269)
C4915 S-(+)-Chlorpheniramine maleate salt H1 histamine receptor antagonist; active isomer.
Chlorpheniramine maleate is clinically used as a topical ointment to treat skin disorders such as sunburn, urticaria, angioedema, pruritus and insect bites.
human ... HRH1(3269)
SML0186 Dp44mT ≥98% (HPLC) Dp44mT (di-2-pyridylketone-4,4,-dimethyl-3-thiosemicarbazone) influences lysosome integrity through copper binding. It induces reactive oxygen species (ROS) generation by redox cycling of iron complex. Dp44mT exhibits anti cancer action by attenuating Ndrg-1 (N-myc downstream regulated 1), a metastasis suppressor protein. It also alters the cyclin family of proteins (A, B, D1, D2,D3 and cyclin-dependent kinase 2) known for cell-cycle regulation. Dp44mT is known to promote apoptosis in neuroepithelioma, melanoma and breast cancer.
Dp44mT is an iron chelator that works as a selective anticancer agent. As other iron chelators it can serve as a therapeutic adjunct to doxorubicin treatment. Additionally Dm44mT possess DNA-damaging activity. It appears that that activity is mediated by top2a inhibition.
SML0147 Drospirenone ≥98% (HPLC) Drospirenone is a fourth-generation progestin that has antimineralocorticoid, and antiandrogenic activity in addition to potent progestogenic activity. In two recent studies drospirenone appeared to double the risk of venous thromboembolism compared to levonorgestrel, although other studies found little added risk.
human ... NR3C2(4306), PGR(5241)
K1751 Ketoprofen ≥98% (TLC) It serves as an efficient drug to treat ankylosing spondylitis, rheumatoid arthritis and osteoarthritis. It also has antipyretic and analgesic effects. Ketoprofen prevents the action of prostaglandin synthetase.
Non-steroidal anti-inflammatory compound that is selective for COX-1.
human ... ALB(213), IL8RA(3577), PTGS1(5742), PTGS2(5743)
M1275 Naproxen sodium 98.0-102.0% Cyclooxygenase (Prostaglandin H synthase 1 and 2) inhibitor.
Naproxen binds preferably to serum albumin. The S-enantiomer of naproxen is 28-fold more potential as an anti-inflammatory drug compared to the R-isomer. The R-isomer is found to be a liver toxin and causes gastrointestinal disorders.
human ... PTGS1(5742), PTGS2(5743)
N7634 Nifedipine ≥98% (HPLC), powder Nifedipine is a L-type Ca2+ channel blocker; and induces apoptosis in human glioblastoma cells. Nifedipine has neuroprotection activity and protects substantia nigra. Nifedipine has antioxidant potential. Nifedipine downregulates inflammatory cytokines like macrophage inflammatory protein-2 (MIP-2), tumor necrosis factor-α (TNF-α). Nifedipine has antihypertensive properties. Nifedipine inhibits extracellular region of adenosine A2a receptor (ADORA2A) gene.
human ... ADORA2A(135), ADORA3(140), CACNA1C(775), CACNA1D(776), CACNA1F(778), CACNA1S(779), CACNA2D1(781), CYP1A2(1544), KCNH1(3756), TTR(7276)
mouse ... Cacna1c(12288)
rat ... Adora1(29290), Adora2a(25369), Cacna1c(24239), Cacna1d(29716), Kcnj1(24521), Kcnn4(65206), Tbxas1(24886)
N3415 Nifurtimox ≥98% (HPLC) Nifurtimox is a nitrofurane derivative used to treat diseases caused by trypanosomes. Nifurtimox was discovered empirically and its mechanism of action is unclear. It is believed that nifurtimox exerts its biological activity through the bioreduction of the nitro-group to a nitro-anion radical which undergoes redox-cycling with molecular oxygen.
N149 Nimodipine Nimodipine enhances the survival of dopaminergic substantia nigra neurons.
Nimodipine is a potent L-type Ca2+ channel antagonist.
human ... ADORA3(140), CACNA1C(775), CACNA1D(776), CACNA1F(778), CACNA1S(779), CACNG1(786), NR3C2(4306)
rat ... Adora1(29290), Adora2a(25369)
N0165 Nisoldipine ≥98% (HPLC) L-type (CaV1.2) calcium channel blocker; dihydropyridine-type calcium channel blocker with selectivity for smooth muscle (CaV1.2b) over cardiac muscle (CaV1.2a). Arterial vasodilator and antihypertensive agent.
human ... CACNA1C(775), CACNA1D(776), CACNA1F(778), CACNA1S(779)
P1636 Phenobarbital Anesthetic; sedative; hypnotic; anticonvulsant
P5178 Phenobarbital sodium salt Phenobarbital, a substituted barbituric acid is an antileptic drug and is not easily eliminated from circulation. It hyperpolarizes the synaptic neuronal membranes by favoring the activation of neuronal postsynaptic GABAA receptors by γ aminobutyric acid (GABA). Phenobarbital is also effective in treating neonatal seizures and status epilepticus.
Sedative; hypnotic; anticonvulsant; enhances GABAergic activity.
Q3251 Quinacrine dihydrochloride ≥90% Non-selective MAO-A/B inhibitor.
Quinacrine has anthelmintic functionality and used in the female sterilization. It is used to treat systemic lupus erythematosus and rheumatic diseases. Apart from malaria, Quinacrine is effective for treating giardia and tapeworm infections. It inhibits nicotinamide adenine dinucleotide phosphate (NADPH) oxidase activity in addition to monoamine oxidase inhibition.
human ... MAOA(4128), MAOB(4129)
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).
human ... ABCB1(5243), CYP2D6(1565), CYP3A4(1576), KCNH1(3756), SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
mouse ... Abcb1a(18671), Abcb1b(18669)
rat ... Cyp2d1(266684), Cyp2d2(25053), Cyp2d3(24303), Cyp2d4v1(171522)
Q0875 Quinidine sulfate salt dihydrate Class IA antiarrhythmic; potassium channel blocker.
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.
R0531 Ramatroban ≥98% (HPLC), solid Ramatroban is used for the treatment of allergic rhinitis as an antagonist of the thromboxane receptor. It is also an antagonist of the DP2 receptor with IC50 values of 100-170 nM. It is more potent at the DP2 receptor than the TP receptor by 4-5 fold. It is therefore a useful tool for the elucidation of PGD2/DP2 function in eosinophils, basophils, and other cells of the TH2 cell-type.
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.
human ... ADRB1(153), ADRB2(154), ADRB3(155), KCNH2(3757)