gpcr agonist-2

GPCR agonist-2 (4-(Cyclopropylamino)-3-nitrobenzoic acid) 是人源 GPCR GPR109B 的激动剂。

7α,25-Dihydroxycholesterol 是一种孤儿 GPCR 受体EBI2 (GPR183)的内源性配体和有效选择性激动剂。它对激活 EBI2 有很强的作用 (EC50=140 pM;Kd=450 pM)。它能够作为一种趋化因子，指导 B 细胞、T 细胞和树突状细胞的迁移。

Tryptophan-cholic acid (Trp-CA) 是一种微生物氨基酸结合胆汁酸（MABAs），是MRGPRE(Mas-related GPCR family member E)的内源性配体和激动剂，进而诱导GLP-1分泌。Tryptophan-cholic acid可以改善糖尿病小鼠的葡萄糖耐量,可用于研究2型糖尿病。

AC-264613 是一种选择性蛋白酶激活受体 (PAR-2) 激动剂，pEC50为 7.5。

MK-8666 Tris is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 Tris has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects.

MK-8666 is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects.