(E/Z)-GSK5182

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(E/Z)-GSK5182  纯度: 98.90%

(E/Z)-GSK5182 是 (E)-GSK5182 和 (Z)-GSK5182 的消旋体。GSK5182 是一种高效选择性，具有口服活性的 ERRγ 反向激动剂，其 IC50 值为 79 nM。GSK5182 还能增加肝癌细胞中 reactive oxyen species (ROS) 的产生。

(E/Z)-GSK5182

(E/Z)-GSK5182 Chemical Structure

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3080 In-stock
5 mg ￥2800 In-stock
10 mg ￥4500 In-stock
50 mg ￥12000 In-stock
100 mg ￥18000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

(E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers. GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM[1]. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma[1][2][3].

分子量

417.54

Formula

C27H31NO3
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (239.50 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3950 mL 11.9749 mL 23.9498 mL
5 mM 0.4790 mL 2.3950 mL 4.7900 mL
10 mM 0.2395 mL 1.1975 mL 2.3950 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Kim JH, et al. Estrogen-related receptor γ is upregulated in liver cancer and its inhibition suppresses livercancer cell proliferation via induction of p21 and p27. Exp Mol Med. 2016 Mar 4;48:e213.

    [2]. Misra J, et al. ERRγ: a Junior Orphan with a Senior Role in Metabolism. Trends Endocrinol Metab. 2017 Apr;28(4):261-272.

    [3]. Kim DK, et al. Inverse agonist of nuclear receptor ERRγ mediates antidiabetic effect through inhibition of hepatic gluconeogenesis. Diabetes. 2013 Sep;62(9):3093-102.

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