mechanism-based inactivator of human cytochrome P450 (CYP) 2B6
CAS：92321-29-4
分子式：C14H21N
分子量：203.3
纯度：98%
存储：Store at -20°C

Background:

KI: 11 microM for 7-(benzyloxy)resorufin O-dealkylation activity of liver microsomes obtained from phenobarbital-induced rats

2-Phenyl-2-(1-piperidinyl)propane is a mechanism-based inactivator of human cytochrome P450 (CYP) 2B6.

The use of selective chemical inhibitors of human cytochrome P450 enzymes is a powerful method by which the relative contributions of different human P450 enzymes to the drug metabolism can be obtained. However, the contribution of CYP2B6 in the metabolism is more challenging due to the lack of a well-established inhibitor.

In vitro: Previous study found that 2-phenyl-2-(1-piperidinyl)propane could inactivate the 7-(benzyloxy)resorufin O-dealkylation activity of liver microsomes obtained from phenobarbital-induced rats. The 7-ethoxy-4-(trifluoromethyl)coumarin O-deethylation activity of purified rat liver P450 2B1 and expressed human P450 2B6 was also inactivated by 2-phenyl-2-(1-piperidinyl)propane in a reconstituted system. With NADPH, the loss of activity was founf to be both time- and concentration-dependent, and followed pseudo first order kinetics. The time for 50% of the P450 2B1 to become inactivated at saturating concentrations of 2-phenyl-2-(1-piperidinyl)propane was