Description
CYP4A11/CYP4F2-IN-2 is a potent and orally active dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC 50 s of 140 nM and 40 nM, respectively. CYP4A11/CYP4F2-IN-2 has potential for the research of renal diseasesIn VitroCYP4A11/CYP4F2-IN-2 (compound 11c) inhibits 20-Hydroxyeicosatetraenoic acid (20-HETE) production from arachidonic acid in human renal microsomes, with an IC 50 of 29 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoCYP4A11/CYP4F2-IN-2 (compound 11c) (0.03-1 mg/kg; a single p.o.) inhibits renal 20-HETE production of rats in a dose-dependent manner. CYP4A11/CYP4F2-IN-2 (0.5 mg/kg; i.v.) exhibits low CL (1430 mL/h/kg), moderate V dss (763 mL/kg), and short T 1/2 (0.424 h) in mice. CYP4A11/CYP4F2-IN-2 (1 mg/kg; i.v.) exhibits low CL (226 mL/h/kg), moderate V dss (839 mL/kg), and T 1/2 (3.01 h) in SD rats. CYP4A11/CYP4F2-IN-2 (1 mg/kg; p.o.) exhibits C max (623 ng/mL), T 1/2 (3.03 h), and high bioavailability (97.7%) in SD rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:CYP4A11 140 nM (IC 50 ) CYP4F2 40 nM (IC 50 )