| 产品描述: | 雌激素/孕激素受体激动剂;Estrogen/progestogen Receptor Agonists;;InformationGSK5182 GSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors.TargetsERRγ |
| 体内研究: |
GSK5182 (40 mg/kg;腹膜内注射;每日一次;25 或 30 天;db/db 小鼠,即饮食诱导的肥胖小鼠) 特异性抑制 ERRγ 的转录活性,并通过抑制肝脏糖异生来抑制肝葡萄糖生成。GSK5182 通过对肝脏糖异生程序进行负向调节,在小鼠模型中发挥抗糖尿病作用。GSK5182 主要通过抑制肝脏葡萄糖生成来使高血糖恢复正常。 |
| 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. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.395 ml |
11.975 ml |
23.95 ml |
| 5 mM |
0.479 ml |
2.395 ml |
4.79 ml |
| 10 mM |
0.239 ml |
1.197 ml |
2.395 ml |
| 50 mM |
0.048 ml |
0.239 ml |
0.479 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |