CINPA1
目录号: PL08423 纯度: ≥99%
CAS No. :102636-74-8
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中文名称
CINPA1
中文别名
化合物 T14969
英文名称
CINPA1
英文别名
Carbamic acid, [5-[(diethylamino)acetyl]-10,11-dihydro-5H-dibenz[b,f]azepin-3-yl]-, ethyl ester;CINPA1;CINPA 1;Ethyl [5-[(diethylamino)acetyl]-10,11-dihydro-5H-dibenz[b,f]azepin-3-yl]carbamate;Carbamic acid, [5-[(diethylamino)acetyl]-10,11-dihydro-5H-dibenz[b,f]azepin-3-yl]-, ethyl ester (9CI)
Cas No.
102636-74-8
分子式
C23H29N3O3
分子量
395.50
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
CINPA1是一种不激活孕烷 X 受体 (PXR) 的,强效、特异性的组成型雄甾烷 (CAR) 抑制剂。CINPA1 能下调 CAR 介导的转录,IC50 值为 ~70 nM。CINPA1 可以作为 CAR 功能研究的分子工具。
生物活性
CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC 50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function.
性状
Solid
IC50 & Target[1][2]
IC50: ~70 nM (CAR)
体外研究(In Vitro)
CINPA1 (1μM ; 24 hours) inhibits CAR-mediated transactivation without activating PXR in HepG2 cells.
CINPA1 is a specific xenobiotic receptor inhibitor and has no cytotoxic effects up to 30 μM.
CINPA1 inhibits CAR-mediated gene expression in primary human hepatocytes, where CAR is endogenously expressed.
CINPA1 does not alter the protein levels or subcellular localization of CAR.
CINPA1 increases corepressor and reduces coactivator interaction with the CAR ligand-binding domain in mammalian two-hybrid assays.
CINPA1 disrupts CAR binding to the promoter regions of target genes in chromatin immunoprecipitation assays.
CINPA1 efficiently inhibits CAR-LBD interaction with the coactivator peptide that suggesting that CINPA1 is a ligand of CAR.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 250 mg/mL (632.13 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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