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GSK5182 是高效选择性,具有口服活性的 ERRγ反向激动剂,其 IC50=79 nM,且不与其他核受体相互作用,包括 ERRα 和 ERα。它还能增加肝癌细胞中 reactive oxyen species (ROS)的产生。
GSK5182 是高效选择性,具有口服活性的 ERRγ反向激动剂,其 IC50=79 nM,且不与其他核受体相互作用,包括 ERRα 和 ERα。它还能增加肝癌细胞中 reactive oxyen species (ROS)的产生。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 397 | 现货 | |
2 mg | ¥ 595 | 现货 | |
5 mg | ¥ 997 | 现货 | |
10 mg | ¥ 1,560 | 现货 | |
25 mg | ¥ 2,790 | 现货 | |
50 mg | ¥ 4,150 | 现货 | |
100 mg | ¥ 5,920 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,090 | 现货 |
产品描述 | GSK5182 is a highly selective inverse estrogen-related receptor γ agonist (IC50 : 79 nM) |
靶点活性 | ERRγ:79 nM (IC50) |
体外活性 | Small interfering RNA (siRNA)-mediated knockdown of ERRγ (siRNA-ERRγ) or an ERRγ inverse agonist, GSK5182, were also used to examine the effects of ERRγ inhibition on the proliferation and growth of a human hepatoma cell line, PLC/PRF/5[1]. |
体内活性 | a hyperinsulinemic-euglycemic clamp study and long-term studies of the antidiabetic effects of GSK5182, the ERRγ-specific inverse agonist, in db/db and DIO mice demonstrated that GSK5182 normalizes hyperglycemia mainly through inhibition of hepatic glucose production[2]. |
细胞实验 | Cell Line:The human hepatoma cell line PLC/PRF/5. Concentration:0 μM, 10 μM, 20 μM. Incubation Time:0 hour, 24 hours, 48 hours, 72 hours |
分子量 | 417.54 |
分子式 | C27H31NO3 |
CAS No. | 877387-37-6 |
Smiles | C(=C(/CCCO)\C1=CC=CC=C1)(\C2=CC=C(OCCN(C)C)C=C2)/C3=CC=C(O)C=C3 |
密度 | 1.132 g/cm3 (Predicted) |
存储 | keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 60 mg/ml (143.7 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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