cyp2b6

Fenofibrate (Lipanthyl) is a PPARα agonist (EC50=30 μM) and is selective. Fenofibrate also inhibits cytochrome P450 isoforms, such as CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4. Fenofibrate exhibits antihyperlipidemic activity.

Memantine hydrochloride (Memantine HCl) is an AMANTADINE derivative that has some dopaminergic effects. Memantine hydrochloride has been proposed as an antiparkinson agent.

2,6-Dimethylquinoline is a natural product extracted from the roots of Peucedantu praeruptorum. 2,6-Dimethylquinoline is an inhibitor of CYP1A2 and CYP2B6 with an IC50 of 3.3 and 480 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.

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

Laromustine (VNP40101M) is a sulfonyl hydrolytic alkylating prodrug used in cancer therapy with significant anticancer activity. Inhibiting thioredoxin reductase can be used to study acute myeloid leukemia.

Clopidogrel hydrogen sulfate ((S)-(+)-Clopidogrel bisulfate) , a selective, high-affinity P2Y12 receptor antagonist, suppressess fibrinogen binding to platelets and platelet adhesion and aggregation.

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)

α-Terpinyl acetate is a natural compound found in several essential oils, is a flavouring agent.

ε-Viniferin (epsilon-Viniferin) a dimer of resveratrol, shows the inhibitory effects of epsilon-viniferin on human CYP1A1, CYP1A2, CYP1B1, CYP2A6, CYP2B6, CYP2E1, CYP3A4 and CYP4A activities.

N-Desmethyl-Apalutamide is a less potent antagonist of the androgen receptor, is an active Apalutamide metabolite.

Apinocaltamide (ACT-709478) is an orally available and selective T-type calcium channel blocker that penetrates the blood-brain barrier (BBB) with IC50=6.4-18nM for Cav3.1, Cav3.2, and Cav3.3, and is commonly used in epilepsy research.

Mertansine is a tubulin inhibitor and an antibody-conjugable maytansinoid alkaloid. The IC50 of Mertansine against HCT-15 and A431 cells is 0.750 and 0.04nM.

DL5050 is a selective agonist for the human constitutive androstane receptor (hCAR). This compound demonstrates superior affinity and selectivity for hCAR by inducing expression of CYP2B6 (the target of hCAR) at the mRNA and protein levels, rather than CYP3A4 (the target of the human pregnane X receptor, hPXR). As a selective hCAR agonist, DL5050 not only serves as a crucial tool molecule for studying hCAR's biological function but also holds potential as a lead compound for the development of therapeutic applications targeting hCAR.

MI-883 is an orally active Constitutive Androstane Receptor (CAR, EC50=73 nM) agonist and a Pregnane X Receptor (PXR, IC50=0.1 μM) antagonist. It enhances CAR LBD assembly (EC50=0.38 µM) and activates the CAR3 variant (EC50=0.074 µM), inducing CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. Additionally, MI-883 inhibits the basal activity of PXR (IC50=2.03 µM) and reduces CYP3A4 mRNA expression in transiently transfected HepG2 cells. It also regulates cholesterol metabolism and bile acid excretion, improving hypercholesterolemia in mouse models.

Mephenytoin (Phenantoin) is an anticonvulsant and a substrate of CYP2C19 and CYP2B6.

HEC72702 is a novel Hepatitis B virus capsid inhibitor, based on clinical candidate GLS4. HEC72702 was found to display no induction of the CYP1A2, CYP3A4, or CYP2B6 enzyme at the high concentration of 10 μM.

8-hydroxy Efavirenz is a major oxidative metabolite of the non-nucleoside reverse transcriptase inhibitor efavirenz . 8-hydroxy Efavirenz is formed when efavirenz is metabolized by the cytochrome P450 (CYP) isoform CYP2B6. It induces apoptosis in rat primary hippocampal neurons and loss of dendritic spines in rat primary hippocampal neuronal cultures when used at a concentration of 0.01 μM.

Fraxinol is a predicted metabolite generated by BioTransformer¹ that is produced by the metabolism of 5, 7-dimethoxy-2h-chromen-2-one. It is generated by cyp1a2, cyp2a6, cyp2b6, cyp2c9, cyp2c19, and cyp2e1 enzymes via an aromatic-hydroxylation-of-fused-be

2-Phenyl-2-(1-piperidinyl)propane (PPP), an analog of phencyclidine, is a chemical compound.

N-desmethyl Apalutamide-d4 is a deuterated compound of N-desmethyl Apalutamide. N-desmethyl Apalutamide has a CAS number of 1332391-11-3. N-Desmethyl-Apalutamide is a less potent antagonist of the androgen receptor, is an active Apalutamide metabolite.

Glycycoumarin is an estrogen agonist, it shows moderate inhibitory effects against CYP1A2 and CYP2B6.

Acetylshikonin can effectively inhibit tumor cells, it can be used to treat hepatocellular carcinoma cells expressing hepatitis B virus X protein (HBX) by inducing ER stress , an oncoprotein from hepatitis B virus. Acetylshikonin inhibits the production of eicosanoid, is due to the attenuation of cytosolic phospholipase A(2) membrane recruitment via the decrease in [Ca(2+)](i) and to the blockade of cyclooxygenase and 5-lipoxygenase activity.

β-Cedrene ((+)-β-Cedrene), a sesquiterpene isolated from both Centaurea kotschyi var. kotschyi and Centaurea kotschyi var. decumbens, exhibits a broad range of biological activities, including antibacterial, anti-inflammatory, antispasmodic, tonic, diuretic, sedative, insecticidal, and antifungal properties. Additionally, β-Cedrene acts as a potent competitive inhibitor of the CYP2B6-mediated bupropion hydroxylase activity, demonstrating a K i value of 1.6 μM [1] [2].