LY2922470 是一种有效、选择性的，口服有效的 GPR40 激动剂，作用于 GPR40、小 GPR40、大 GPR40 EC50 值分别为 7 nM? nM? nM。LY2922470 可降低血糖水平，同时显著增加胰岛素和 GLP-1，具有治 2 型糖尿病 (T2DM) 的潜力、div>
| Cas No. |
1423018-12-5 |
| Canonical SMILES |
COC1=C(N(CC2=CC=C(COC3=CC=C([C@@H](C#CC)CC(O)=O)C=C3)S2)CCC4)C4=CC=C1 |
| 分子弎/td> |
C28H29NO4S |
| 分子野/td> |
475.6 |
| 溶解?/td> |
DMSO: 125 mg/mL (262.83 mM) |
| 储存条件 |
Store at -20C |
| General tips |
For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while. |
| Shipping Condition |
Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 |
LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM)[1]. EC50:7 nM (human GPR40), 1 nM (mouse GPR40), 3 nM (rat GPR40)[1] [1]. Hamdouchi C, et al. The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). J Med Chem. 2016 Dec 22;59(24):10891-10916. |
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