cyp3a activity

1,3,7-Trimethyluric acid, a purine alkaloid, occurs as a minor metabolite of caffeine in humans. It functions as an antioxidant with the ability to scavenge hydroxyl radicals and offers protective benefits against lipid peroxidation in erythrocyte membranes.

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.

Schisandrin A, a primary active component extracted from the traditional Eastern medicine Schisandra chinensis, inhibits CYP3A activity, with an IC50 of 6.60 μM and a Ki of 5.83 μM.

1. Dauricine has pulmonary toxicity, can produce pulmonary injury in CD-1 mice by the metabolism of Dauricine mediated by CYP3A. 2. Dauricinec can pass the blood-brain barrier, and that P-glycoprotein has an important role in the transportation of Dauricine across the blood-brain barrier. 3. Dauricine may has anti-tumor effect, can inhibit tumor cells in urinary system and colon cancer cell proliferation, invasion; induce cell apoptosis by suppressing NF-kappaB activity and the expression profile of its downstream genes.

11α-Hydroxy Testosterone, a testosterone metabolite, is synthesized by the cytochrome P450 (CYP) isoform CYP3A.1, and can alternatively be produced from testosterone by a CYP107A1 mutant or from 11α-hydroxy progesterone by the fungus B. bassiana.2,3 The biological activity of 11α-Hydroxy Testosterone remains unclear.

Dauricine (Standard) is a reference standard for research and analysis in studies involving Dauricine. 1. Dauricine has pulmonary toxicity, can produce pulmonary injury in CD-1 mice by the metabolism of Dauricine mediated by CYP3A. 2. Dauricinec can pass the blood-brain barrier, and that P-glycoprotein has an important role in the transportation of Dauricine across the blood-brain barrier. 3. Dauricine may has anti-tumor effect, can inhibit tumor cells in urinary system and colon cancer cell proliferation, invasion; induce cell apoptosis by suppressing NF-kappaB activity and the expression profile of its downstream genes.

6',7'-Dihydroxybergamottin is a potent inhibitor of CYP3A activity, and may be primarily responsible for the effects of grapefruit juice on cytochrome P450 activity in humans.