产品描述:
CINPA1 is a constitutive androstane receptor (CAR) antagonist (IC50 = 70 nM in a reporter assay).{48670} It is selective for CAR over the nuclear receptors GR, FXR, LXRα, LXRβ, PPARγ, RXRα, and RXRβ at 18 μM, but also antagonizes the human pregnane X receptor (PXR; IC50 = 6.6 μM). CINPA1 (0.3-5 μM) inhibits CAR transactivation of CYP2B6 induced by CITCO (Item No. 16027) in primary human hepatocytes.