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CAS No.: 102636-74-8

CINPA1 Catalog No. CSN23907

CINPA1 is a CAR inhibitor capable of reducing CAR-mediated transcription with an IC50 of ∼70 nM.

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靶点选择性

生物活性

实验方案

技术信息

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]
动物研究
剂量
Mice: 1 mg/kg - 50 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 1 mg/kg - 50 mg/kg^[3] (i.p.)
给药途径	i.p.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5285 mL
- 12.6424 mL
- 25.2848 mL
- 5 mM
- 0.5057 mL
- 2.5285 mL
- 5.0570 mL
- 10 mM
- 0.2528 mL
- 1.2642 mL
- 2.5285 mL

技术信息

CAS号

102636-74-8

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H29N3O3

运输

蓝冰

分子量

395.49

别名

溶解度

DMSO	240.0 mg/mL (606.8 mM) warming

动物实验配方

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