Cytochrome P450 (CYP) inhibition assay (IC50)

Cytochrome P450 (CYP) is a superfamily of heme-containing enzymes, which mediate the inactivation and metabolism of many drugs and endogenous substances. Compounds that inhibit P450 may cause the accumulation of toxicity of other substrates. CYP inhibition profile analysis examine the effects of test compounds on the metabolism of five major human metabolic CYP substrates: 1A2, 2B6, 2C9, 2D6, and 3A4. The levels of labeled substrates and metabolites of each CYP isoform are measured by LC/MS/MS in the presence and absence of test compounds.

Cytochrome P450 (CYP) inhibition assay Protocol (Single Point)

Compound test concentration 10µM,0µM
CYP450 isoforms 1A2,3A4, 2C9, 2C19, 2D6
Microsome concentration 0.05-0.5mg/mL
Cofactor NADPH
Incubation duration 5-40分钟
IC50 calculation
Data Interpretation IC50<1 µM Strong Inhibitor
1µM IC50>10 µM Weak or Non Inhibiotr
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