CITCO

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Chemical Structure| 338404-52-7 同义名 : -
CAS号 : 338404-52-7
货号 : A1167756
分子式 : C19H12Cl3N3OS
纯度 : 99%+
分子量 : 436.74
MDL号 : MFCD00139608
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(57.24 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
生物活性
描述 The constitutive androstane receptor (CAR) is a xenobiotic sensor expressed in hepatocytes that activates genes involved in drug metabolism, lipid homeostasis, and cell proliferation[1]. In vitro, CAR activation accelerated intestinal epithelial wound healing by enhancing cell migration[2]. CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49 nM over pregnane X receptor (PXR). CITCO (1-50 μM; 48 hours) results in a dose-dependent inhibition of viable cell count and proliferation in both T98G and U87MG glioma and BTSCs. CITCO (2.5, 5 μM; 48 hours) induces cell cycle arrest differentially in different BTSCs in culture, but not in normal astrocytes. CITCO (2.5-10 μM; 48 hours) induces apoptosis in BTSCs in culture (dose dependently), and causes the T98G and U87MG glioma and BTSCs expressing very low levels of CAR protein. CITCO (intraperitoneal; on days 22, 24, 26, 30 and 36) with 25 μg results a significant decrease in tumour growth, which further decreases to an undetectable level after treatment with 100 μg CITCO[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.29mL

0.46mL

0.23mL

11.45mL

2.29mL

1.14mL

22.90mL

4.58mL

2.29mL
参考文献

[1]Michael McMahon,et al. Constitutive androstane receptor 1 is constitutively bound to chromatin and 'primed' for transactivation in hepatocytes. Mol Pharmacol. 2019. 95(1), 97-105.

[2]Grace M Hudson,et al. Constitutive androstane receptor regulates the intestinal mucosal response to injury. Br J Pharmacol. 2017. 174(12), 1857-1871.

[3]Chakraborty S, et al. Constitutive androstane receptor agonist CITCO inhibits growth and expansion of brain tumour stem cells. Br J Cancer. 2011. 104(3), 448-59.