cyp3a5

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.

Clobetasol propionate (CGP9555) exerts its effect by binding to cytoplasmic glucocorticoid receptors and subsequently activates glucocorticoid receptor-mediated gene expression. This results in the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Clobetasol Propionate is the propionate salt form of clobetasol, a topical synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive properties. Specifically, clobetasol propionate appears to induce phospholipase A2 inhibitory proteins, thereby controlling the release of the inflammatory precursor arachidonic acid from membrane phospholipids by phospholipase A2.

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.

N-Desethyl vardenafil is a metabolite of vardenafil , a phosphodiesterase 5 inhibitor, that is formed by the action of cytochrome P450 (CYP)3A4 and CYP3A5.

The naturally-occurring estrogens are estrone , estradiol , and estriol . 16α-hydroxy Estrone (16α-OHE1) is a hydroxylated metabolite of E1 as well as an interconversion product with E2. E1 is 16α-hydroxylated by cytochrome P450 (CYP) isoforms, including CYP1A1, CYP3A5, CYP3A4, and CYP3A7, with CYP3A5 being breast-specific. 16α-OHE1 is sulphatized or glucuronidated before excretion. It is increased in rheumatoid arthritis and decreased by physical activity. Unlike the parent estrogens and other hydroxylated metabolites of E1, 16α-OHE1 binds covalently and persistently activates estrogen receptors. In addition, this metabolite increases cell proliferation and does not suppress TNF-α secretion, whereas other estrogen metabolites are not pro-proliferative and have marked effects on TNF-α secretion. The levels of 16α-OHE1 are increased in some forms of hormone therapy. Because hormone therapy increases breast cancer risk, 16α-OHE1 has been implicated as a risk factor for breast cancer, although supportive data remains elusive.

N-Desmethyl sildenafil is a major metabolite of sildenafil . N-Desmethyl sildenafil is formed via oxidative metabolism of sildenafil by the cytochrome (CYP) P450 isoforms CYP3A4, CYP3A5, and CYP3A7.

(3S)-hydroxy Quinidine is an active quinidine metabolite. Quinidine, an antiarrhythmic agent, undergoes rapid first-pass metabolism by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2C9, CYP2E1, and CYP3A5, with CYP3A4 being the most active enzyme in the (3S)-hydroxy quinidine formation. (3S)-hydroxy Quinidine prolongs repolarization of canine Purkinje fibers in vitro and prevents ventricular fibrillation and ventricular tachycardia after coronary reperfusion in isolated rat hearts in a dose-dependent manner.

Dehydro Nifedipine (BAY-b 4759) is the main metabolite of nifedipine in human plasma. Dehydro Nifedipine inhibits glucose uptake in PC-12 cells with an IC50 value of 130 μM. Nifedipine is a calcium channel blocker used in the treatment of hypertension and angina. Dehydronifedipine is formed when it is metabolized by cytochrome P450 (CYP) isomers CYP3A4 and CYP3A5.

6β-hydroxy Eplerenone is a major metabolite of the mineralocorticoid receptor antagonist eplerenone .1 It is formed from eplerenone by the cytochrome P450 (CYP) isoform CYP3A4. |1. Cook, C.S., Berry, L.M., Kim, D.H., et al. Involvement of CYP3A in the metabolism of eplerenone in humans and dogs: Differential metabolism by CYP3A4 and CYP3A5. Drug Metab. Dispos. 30(12), 1344-1351 (2002).

6β-Hydroxy Prednisolone, the active metabolite of prednisone and a derivative of prednisolone, is predominantly synthesized via the cytochrome P450 (CYP) isoform CYP3A4 and, to a lesser extent, CYP3A5.

Desethoxy quetiapine, an active metabolite of the atypical antipsychotic quetiapine, primarily forms through the action of the cytochrome P450 (CYP) isoform CYP3A5. This compound binds to dopamine D2 receptors with an IC50 value of 1,330 nM. In vivo, desethoxy quetiapine at dosages of 20 and 40 mg kg mitigates dopamine receptor agonist apomorphine-induced climbing behavior and ameliorates swimming deficits in mice, showcasing its potential modulatory effects on dopamine-mediated behaviors.