| Description | CINPA1 (CINPA 1) is a selective inhibitor of constitutive androstane receptor (CAR) with an IC50 of 70 nM for CAR-mediated transcription. CINPA1 can be used in studies about CAR function. |
| In vitro | CINPA1是一种特异性异生体受体抑制剂，在30 μM浓度下无细胞毒性效应。CINPA1能够抑制初级人类肝细胞中CAR介导的基因表达，其中CAR为内源性表达，且有效阻断CAR-LBD与共激活肽的相互作用。在HepG2细胞中，CINPA1（1μM）抑制CAR介导的转激活作用，而不激活孕烯X受体（PXR）。在哺乳动物双杂交实验中，CINPA1增强了与CAR配体结合域相互作用的核抑制剂，并减少了共激活剂的作用。在染色质免疫沉淀实验中，CINPA1干扰了CAR与目标基因启动子区域的结合[1]。 |
| Target activity | CAR:~70 nM |
| Synonyms | CINPA-1, CINPA 1 |
| molecular weight | 395.49 |
| Molecular formula | C23H29N3O3 |
| CAS | 102636-74-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 200 mg/mL (505.7 mM), Sonication is recommended. |
| References | 1. Cherian MT, et al. CINPA1 is an inhibitor of constitutive androstane receptor that does not activate pregnane X receptor. Mol Pharmacol. 2015 May;87(5):878-89. |