GSK706 is a novel effective agonist of the GPR119.

Firuglipel is an orally available and selective agonist of GPR119.

FFA2 allosteric agonist. Inhibits forskolin-induced cAMP increase and stimulates 35SGTPγS binding in biochemical assays (pEC50 values are 6.9 and 7.23, respectively). Binds at allosteric binding site. In functional assays, displays positive allosteric modulation of FFA-induced Gi signaling and negative allosteric modulation of FFA-induced Gq/G11 signaling. Inhibits lipolytic effect of isoproterenol (pEC50 = 5.03) and induces migration of human neutrophils in vitro. Bolognini et al (2016) A novel allosteric activator of free fatty acid 2 receptor displays unique Gi-functional bias. J.Biol.Chem. 291 18915 PMID:27385588 |Sergeev et al (2017) A single extracellular amino acid in free fatty acid receptor 2 defines antagonist species selectivity and G protein selection bias. Sci.Rep. 7 13741 PMID:29061999

GPR109 receptor agonist-2 (Compound 5)作为选择性GPR109a激动剂，表现出pEC50值为5.53。

FFA3 agonist 1为一种FFA3（游离脂肪酸受体 3）激动剂，功能为通过激活FFA3以调节肠道微生物群的健康效应。

PSN 375963 hydrochloride 是一种有效的GPR119激动剂，对人和小鼠GPR119的EC50分别为 8.4 和 7.9 μM。PSN 375963 hydrochloride 表现出与内源性油酰乙醇酰胺 (OEA) 相似的效力。

Urotensin-II (UT) receptor ligand; behaves as a silent antagonist in most in vitro assays and in vivo, but does retain small residual agonist activity under certain conditions in some assays. Competitively antagonizes U-II induced contractions in the rat

TP-051 是一种高效且具有高度选择性的 FFAR1 激动剂，对人源 FFAR1 表现出 Ki = 16 nM 的亲和力，并已证明其可增强大鼠胰岛瘤细胞中的胰岛素分泌。TP-051 被广泛用作化学探针、 2 型糖尿病和代谢疾病中游离脂肪酸受体介导的信号通路的相关研究。

GPR35 agonist 4 (compound 10) 是一种有效的GPR35激动剂，其效价 pEC50为 5.86。GPR35 agonist 4 在人和大鼠 GPR35 中均显示高效价。精氨酸 3.36 的突变体可消除 GPR35 agonist 4 的激动剂功能。