规格: | 98% |
分子量: | 395.5 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
Background:
CINPA1 is a constitutive androstane receptor (CAR) antagonist (IC50 = 70 nM in a reporter assay).1 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 in primary human hepatocytes.
|1. Cherian, M.T., Lin, W., Wu, J., et al. CINPA1 is an inhibitor of constitutive androstane receptor that does not activate pregnane X receptor. Mol. Pharmacol. 87(5), 878-889 (2015).