CITCO
组成型雄激素受体(CAR)激动剂
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 5mg | ¥1200.00 | 10-15工作日发货 | |
| 10mg | ¥1887.00 | 10-15工作日发货 | |
| 25mg | ¥3430.00 | 10-15工作日发货 |
特色产品
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
CITCO, an imidazothiazole derivative, is a selective agonist of human CAR, with an EC50 value of 49 nM and > 50-fold selectivity to CAR over pregnane X receptor (PXR), and no activity on other nuclear receptors. Upon activation with specific agonists, CAR translocates into the nucleus and binds to the response elements as monomers or CAR/RXR heterodimers. The CAR functions as a xenobiotic receptor, involved in detoxification and clearance of toxic substances from the liver. In addition, activation with selective CAR agonists such as CITCO has also been shown to inhibit growth and expansion of brain tumor stem cells.
Reference:
1. Chakraborty S, Kanakasabai S, Bright JJ. Constitutive androstane receptor agonist CITCO inhibits growth and expansion of brain tumour stem cells. British Journal of Cancer, 2011, 104(3): 448-459.
产品性质
| 物理外观 | A crystalline solid |
| CAS号 | 338404-52-7 |
| 分子式 | C19H12Cl3N3OS |
| 分子量 | 436.74 |
| 化学名称 | (E)-6-(4-chlorophenyl)imidazo[2,1-b]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl) oxime |
| 溶解度 | Soluble in DMSO |
| SMILES | Clc(cc1)ccc1-c1c(/C=N/OCc(cc2)cc(Cl)c2Cl)[n](cc[s]2)c2n1 |
| 存储条件 | -20°C干燥 |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
| 生物活性描述 | CITCO 是一种咪唑噻唑衍生物;是一种选择性促性雄烷受体 (CAR) 激动剂。CITCO 可抑制脑肿瘤干细胞(BTSCs)的生长和扩增;对孕烷 X 受体(PXR)的 EC50 值为 49.nM;对其他核受体无活性。 |
生物相关数据
质量控制
操作说明
APExBIO 顾客使用本产品发表的 2 篇科研文献
- 1. Liu M, Zhu D, et al. "Berberine Promotes OATP1B1 Expression and Rosuvastatin Uptake by Inducing Nuclear Translocation of FXR and LXRα." Front Pharmacol. 2020;11:375. PMID:32292349
- 2. Hu Q, Yao N, et al. "Constitutiveandrostane receptor weakens the induction of panaxytriol on CYP3A4 by repressing the activation of pregnane X receptor." Biochem Pharmacol. 2019 Jan;159:32-39. PMID:30414935



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