Furafylline was a potent, non-competitive inhibitor of high affinity phenacetin O-deethylase activity of microsomal fractions of human liver, a reaction catalysed by P450IA2, with an IC50 value of 0.07 microM. Furafylline had either very little or no effect on human monooxygenase activities catalysed by other isoenzymes of P450, including P450IID1, P450IIC, P450IIA.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO >10 mg/mL|
|Related Cytochrome P450 (e.g. CYP17) Products|
Naringin, a flavanone glycoside, exerts various of pharmacological effects such as blood lipid lowering, antioxidant activity, anticancer activity, and inhibition of cytochrome P450 enzymes.
Tebuconazole is an agricultural azole fungicide that also inhibits CYP51 for Candida albicans CYP51 (CaCYP51) and truncated human CYP51 (Δ60HsCYP51). IC50 The values are 0.9 and 1.3 μM, respectively.
Uniconazole is a plant growth regulator that inhibits cytochrome P450 707As (Ki=68 nM) plays a role, which is a family of enzymes that separate abscisic acid and therefore inhibits the biosynthesis of gibberellin and sterols.
Dihydroestherol (Dihydromethysticin) kava lactone, with induced CYP3A23 activity.
Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM.
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