产品
编 号:F397375
分子式:C28H40Cl2N2O4
分子量:539.53
产品类型
结构图
CAS No: 5853-29-2
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产品详情
生物活性:
Cephaeline dihydrochloride is a selective CYP2D6 inhibtor with an IC50 of 121 μM.
体外研究:
CYP2D6 reveals the highest metabolic activity for the generation of 9-O-demethylEmetine, whereas this enzyme also shows a significant metabolic activity for the generation of Cephaeline. The IC50s of Cephaeline against CYP2C9, CYP2D6 and CYP3A4 is over 1000, 121 and 1000 μM, respectively. Further experiments are performed to determine inhibition constants (Ki) for Cephaeline on the CYP2D6 and CYP3A4 activities Graphic analysis of Dixon plots at various Cephaeline concentrations for each of the two CYP enzyme assays yield Kis of 54 and 355 μM for CYP2D6 and CYP3A4, respectively.