GSK5182|877387-37-6|-陌孚医药/Medlife

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GSK5182

目录号: PL01879 纯度: ≥99%

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 不与其他核受体相互作用，包括 ERRα 和 ERα。GSK5182 还能增加肝癌细胞中 reactive oxyen species (ROS) 的产生。

CAS No. :877387-37-6

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中文名称	GSK5182
英文名称	GSK5182
英文别名	GSK5182;GSK 5182;(Z)-4-(1-{4-[2-(DIMETHYLAMINO)ETHOXY]PHENYL}-5-HYDROXY-2-PHENYLPENT-1-ENYL)PHENOL;TXF;4-[(1Z)-1-{4-[2-(dimethylamino)ethoxy]phenyl}-5-hydroxy-2-phenylpent-1-en-1-yl]phenol;2ewp;GTPL8908;BDBM22435;AOB1629;4-[(z)-1-[4-(2-dimethylaminoethyloxy)phenyl]-hydroxy-2-phenylpent-1-enyl]phenol;4-[(Z)-1-[4-(2-dimethylaminoethyloxy)phenyl]-5-hydroxy-2-phenylpent-1-enyl]pheno
Cas No.	877387-37-6
分子式	C₂₇H₃₁NO₃
分子量	417.54
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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 不与其他核受体相互作用，包括 ERRα 和 ERα。GSK5182 还能增加肝癌细胞中 reactive oxyen species (ROS) 的产生。
生物活性	GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC 50 of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma (HCC).
性状	Solid
IC50 & Target[1][2]	ERRγ 79 nM (IC50) Reactive Oxygen Species pan>&nbs
体外研究(In Vitro)	GSK5182 (0-20 μM; 0-hours; PLC/PRF/5 cells) treatment leads to a significant and dose-dependent reduction in the number of proliferating PLC/PRF/5 cells. GSK5182 (0-20 μM; 24 hours; PLC/PRF/5 cells) treatment also causes a dose-dependent increase in the expression of p21 and p27 while at the same time reducing the level of phosphorylated retinoblastoma protein (p-pRb). GSK5182 (10-20 μM; PLC/PRF/5 cells) treatment induces cell cycle arrest at G1 phase, which in turn induces a corresponding dose-dependent reduction in the percentage of cells in S phase. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	GSK5182 (40 mg/kg; intraperitoneal injection; every day; 25 or 30 days; db/db mice, diet-induced obesity mice) specifically inhibits the transcriptional activity of ERRγ, and suppresses hepatic glucose production through inhibition of hepatic gluconeogenesis. GSK5182 elicits anti-diabetic effects in mouse models via negative regulation of the hepatic gluconeogenesis program. GSK5182 normalizes hyperglycemia mainly through inhibition of hepatic glucose production. has not independently confirmed the accuracy of these methods. They are for reference only.
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
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.

溶解度数据	In Vitro: DMSO : 25 mg/mL (59.87 mM; ultrasonic and warming and heat to 80°C)配制储备液

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