S89479 |
GPR40/FFAR1 modulator 1 |
源叶(MedMol) | 98% |
- 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
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输入产品批号:
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)