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。
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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]. |
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 |
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 |
动物实验配方 |