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CINPA1

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Chemical Structure| 102636-74-8 同义名 : -
CAS号 : 102636-74-8
货号 : A1145760
分子式 : C23H29N3O3
纯度 : 99+%
分子量 : 395.495
MDL号 : MFCD00288296
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(632.12 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 CINPA1 is a selective CAR (Constitutive androstane receptor) with IC50 value of ~70nM for inhibition of CAR-mediated gene expression in primary human hepatocytes. It showed no activity on PXR and did not alter the protein levels or subcellular localization of CAR. CINPA1 attenuated CAR-mediated gene expression, including CYP2B6 and CYP3A4 at concentration of 1μM or 5μM at different cells expressing CAR post 24h or 48h.
作用机制 CINPA1 could reside in the ligand-binding pocket to stabilize the CAR-LBD (ligand-binding domain) in a more rigid, less fluid state and disrupt CAR binding to the DNA response elements at promoter regions of target gene.[1][2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.64mL

2.53mL

1.26mL

25.28mL

5.06mL

2.53mL
参考文献

[1]Cherian MT, Lin W, 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.

[2]Cherian MT, Chai SC, et al. CINPA1 binds directly to constitutive androstane receptor and inhibits its activity. Biochem Pharmacol. 2018 Jun;152:211-223.