CYP3 Substrate

7-Benzyloxy-4-(trifluoromethyl) coumarin (7-BFC) is a coumarin-based fluorescent substrate. 7-Benzyloxy-4-(trifluoromethyl) coumarin serves as a substrate for cDNA-expressed CYP1A2 and CYP3A4, and is metabolized into 7-hydroxy-4-trifluoromethylcoumarin (HFC). 7-Benzyloxy-4-(trifluoromethyl) coumarin supports metabolic studies of cytochrome P450 subtypes via its fluorescent metabolite.

Praeruptorin A ((+)-Praeruptorin A) is an orally active isomer of (±)-Praeruptorin A (HY-N0081). Praeruptorin A also acts as a Calcium channel blocker. Praeruptorin A can be isolated from Peucedanum. Praeruptorin A serves as a substrate for CYP3A4. Praeruptorin A downregulates NMDA receptors containing GluN2B and inhibits neuronal Apoptosis. Praeruptorin A mediates vasodilation, inhibits vascular hypertrophy and reduces blood pressure. Praeruptorin A can be used in research related to neurological diseases, myocardial ischemia, heart failure, exertional angina, renovascular hypertension and spontaneous hypertension.

Dimethocaine (Larocaine) is a cocaine derivative and ester-type local anesthetic. Dimethocaine is metabolized by hP450 1A2, 2C19, 2D6, and 3A4 in vitro. Dimethocaine exhibits locomotor-promoting, reinforcing, and anxiogenic effects.

HN0037 is a selective, orally active Helicase-primase inhibitor. HN0037 is mainly metabolized by CYP3A4. HN0037 inhibits HSV replication by targeting the viral helicase-primase complex, which consists of three proteins encoded by UL5 (helicase), UL52 (primase), and UL8 (scaffold protein that promotes primer synthesis).

BI-11634 is an orally active factor Xa inhibitor and a CYP3A4 substrate. The apparent K_m values for BI-11634 metabolism are 23 μM in human liver microsomes (HLMs) and 7.6 μM with recombinant CYP3A4. BI-11634 can be used for thromboembolic disease and CYP3A4-mediated drug metabolism research.