Murayama, Norie published the artcileAssessment of multiple cytochrome P450 activities in metabolically inactivated human liver microsomes and roles of P450 2C isoforms in reaction phenotyping studies, COA of Formula: C13H8Cl2O4S, the main research area is cytochrome P450 liver microsome phenotype; celecoxib; diclofenac; omeprazole; troglitazone; warfarin.
The fraction of substrate metabolized (fm) can be used to estimate drug interactions and can be determined by comparison of the intrinsic clearances (CLint) of victim drugs obtained from inhibited and uninhibited hepatic enzymes. Com. available human liver microsomes were recently developed in which one cytochrome P 450 (P 450) isoform is selectively inactivated. These inactivated liver microsomes were used to evaluate the roles of P 450 2C isoforms in the depletion and oxidation of probe substrates. Determination of CLint with sets of control and P 450 2C9-inactivated liver microsomes yielded fm,P4502C9 values of 0.69-1.0 for celecoxib, diclofenac and warfarin. Selectively inactivated liver microsomes were thereby shown to be potentially useful for determining the in vitro fm values for major P 450 2C9 contributions to substrate oxidations R-, S- and racemic omeprazole and troglitazone oxidation activities by liver microsomes at multiple substrate concentrations were suppressed by 26-36% and 22-50%, resp., when P 450 2C19- and 2C8-inactivated liver microsomes were used in place of control liver microsomes. This study provides important information to help elucidate the different roles of P 450 isoforms in metabolite formation at different substrate concentrations The data obtained allow the fractions metabolized to be calculated for victim drugs.
Biopharmaceutics & Drug Disposition published new progress about Animal gene, CYP3A4 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, COA of Formula: C13H8Cl2O4S.
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem