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CITCO {[allProObj[0].p_purity_real_show]}

货号:A1167756

CITCO是一种选择性的构成性雄烯受体(CAR)激动剂。它抑制大脑肿瘤干细胞(BTSCs)的生长和扩展,EC50为49 nM,相对于孕烯X受体(PXR)具有选择性,对其他核受体无活性。

CITCO 化学结构 CAS号:338404-52-7
CITCO 化学结构
CAS号:338404-52-7
CITCO 3D分子结构
CAS号:338404-52-7
CITCO 化学结构 CAS号:338404-52-7
CITCO 3D分子结构 CAS号:338404-52-7
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CITCO 纯度/质量文件 产品仅供科研

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CITCO 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].

CITCO 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.

CITCO 实验方案

计算器
存储液制备 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

CITCO 技术信息

CAS号338404-52-7
分子式C19H12Cl3N3OS
分子量 436.742
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

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

溶解方案

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

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