cyp3a4

PF-4981517 (CYP3cide) is a efficient, specific and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC 50 values for CYP3A activity are 0.03 μM,17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. PF-4981517 is able to be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug Metabolism.

Ketoconazole (R-41400), a CYP3A4 inhibitor, is an imidazole anti-fungal agent.

Verapamil hydrochloride (Verapamil HCl) is a calcium channel blocker that is a class IV anti-arrhythmia agent.

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.

Clarithromycin (A-56268) is a Macrolide Antimicrobial. The mechanism of action of clarithromycin is as a Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 3A Inhibitor, and P-Glycoprotein Inhibitor. The chemical classification of clarithromycin is Macrolides.

Verapamil (CP-16533-1) is a calcium channel blocker and an orally active and effective inhibitor of P-gp. Verapamil inhibits CYP3A4 and can be used in studies about the treatment of high blood pressure, heart arrhythmias, and angina research.

Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor P2X7. Tanshinone IIA sulfonate sodium (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats.

Piperine (Bioperine) , a alkaloid, has been used in trials studying the treatment of multiple myeloma and deglutition disorders.

Tetrahydrocurcumin (HZIV 81-2), a major metabolite of curcumin, has strong antioxidant and cardioprotective properties.

Stiripentol (BCX2600) (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59/0.516 μM and IC50 of 1.58/3.29 μM, respectively.

Cedrol is a cedrane sesquiterpenoid and a tertiary alcohol,Cedrol inhibits the cytochrome P450 (CYP) isoforms CYP2B6 and CYP3A4 (Kis = 0.9 and 3.4 μM, respectively)

Germacrone is extracted from Curcuma zedoaria and has anti-inflammatory, anti-androgenic and antiviral activities. It also inhibits the proliferation of glioma cells by promoting apoptosis.

Cletoquine is a major active metabolite of Hydroxychloroquine. Cletoquine has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune disease treatment.

BMS-819881, a melanin-concentrating hormone receptor 1 (MCHR1) antagonist, binds rat MCHR1 with a Ki of 7 nM, and is selective and potent for CYP3A4 activity with an EC50 of 13 μM.

Esomeprazole is the S-isomer of omeprazole, inhibits the lysosomal cysteine protease legumain to prevent cancer metastasis. Esomeprazole is a proton pump inhibitors (PPI).

1. Bergaptol (4-Hydroxybergapten) shows very good radical scavenging activity. 2. Bergaptol is a potent inhibitor of debenzylation activity of CYP3A4 enzyme.

Curdione ((+)-Curdione) inhibits CYP3A4 activity and the production of prostaglandin E2. Curdione inhibits proliferation of MCF-7 cells by inducing apoptosis. Curdione may be a candidate for anti-inflammatory and Y chemopreventive agents.

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.

alpha-Asarone (trans-Asarone) is a psychoactive compound with antidepressant-like activity in mice.

Rosavin (Rosavidin) has antidepressant and anxiolytic actions, helps balance all the neurotransmitters.

TAK-715 is a p38 MAPK inhibitor for p38α.

Pyributicarb (TSH-888) is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).

Chalepensin, a furanocoumarin isolated from the rutaceae plant Ruta chalepensis L., is a selective CYP2A6 inhibitor, inhibiting CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4.Chalepensin exhibits Chalepensin j has antiprotozoal activity and inhibits methicillin-resistant Staphylococcus aureus (MRSA) with MIC values in the range of 32-128 μg/mL.

Norfluoxetine Hydrochloride (Norfluoxetine HCl) is an active metabolite of fluoxetine. Fluoxetine is an antidepressant drug.