| 产品描述： | GPR40/FFAR1 modulator 1 is a Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1) agonist and allosteric modulator. |
| 靶点： |
GPR |
| 体外研究： |
The long-chain fatty acid receptor FFAR1/GPR40 binds agonists in both an interhelical site between the extracellular segments of transmembrane helix (TM)-III and TM-IV and a lipid-exposed groove between the intracellular segments of these helices. Molecular dynamics simulations of FFAR1 with agonist removed demonstrated a major rearrangement of the polar and charged anchor point residues for the carboxylic acid moiety of the agonist in the interhelical site, which was associated with closure of a neighboring, solvent-exposed pocket between the extracellular poles of TM-I, TM-II, and TM-VII. A synthetic compound designed to bind in this pocket, and thereby prevent its closure, was identified through structure-based virtual screening and shown to function both as an agonist and as an allosteric modulator of receptor activation |
| 参考文献： |
1. Lückmann M, et al. Molecular dynamics-guided discovery of an ago-allosteric modulator for GPR40/FFAR1. Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):7123-7128. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.568 ml |
12.84 ml |
25.68 ml |
| 5 mM |
0.514 ml |
2.568 ml |
5.136 ml |
| 10 mM |
0.257 ml |
1.284 ml |
2.568 ml |
| 50 mM |
0.051 ml |
0.257 ml |
0.514 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京