g protein-coupled receptor 119

APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119, respectively.

MBX-2982 is a selective, orally available GPR119 agonist used in the treatment of diabetes.

AS1269574 (AS 1269574) is a potent, orally available GPR119 agonist with potential for type 2 diabetes research.

PSN 375963 (PSN 375963 hydrochloride) hydrochloride is a synthetic agonist of the endogenous ligand for GPR119.

MK-8282 is an effective G-Protein-Coupled Receptor 119 agonist for the treatment of Type 2 Diabetes.

GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2.

AS-1669058 is a G-protein-coupled receptor 119 (GPR119) agonist for the treatment of type 2 diabetes mellitus.

APD597 (JNJ-38431055) is a GPR119 agonist, used in the treatment of type 2 diabetes.

AS-1669058 free base is a G-protein-coupled receptor 119 (GPR119) agonist used to as new drug to treat type 2 diabetes.

Azenosertib (ZN-c3) is an orally active, specific GPR119 agonist. Azenosertib (ZN-c3) stimulates cell proliferation and improves pancreatic β-cell function. [1]

Tirzepatide acts as an agonist for both the glucagon-like peptide 1 receptor (GLP-1R) and G protein-coupled receptor 119 (GPR119), effectively inducing cAMP production in HEK293 cells that express either human GLP-1R or GPR119, with EC50 values of 6.54 and 1.01 nM, respectively. Additionally, at a concentration of 100 nM, it triggers receptor internalization in these cells. In vivo studies demonstrate that tirzepatide, administered at 10 nmol/kg per day, significantly reduces body weight, food intake, as well as plasma and hepatic triglyceride levels, free fatty acids (FFAs), leptin, and blood glucose in mice with high-fat diet-induced obesity. Furthermore, a dose of 50 nmol/kg every three days prevents an increase in eosinophils and lymphocytes in the bronchoalveolar lavage fluid (BALF) and inhibits bronchoconstriction prompted by methacholine in mice models of both asthma and diabetes, indicating its potential in treating type 2 diabetes mellitus.

5(S)-HEPE, an active metabolite of eicosapentaenoic acid (EPA), is produced via the action of 5-lipoxygenase (5-LO). This compound functions as an agonist for G protein-coupled receptor 119 (GPR119), promoting cAMP accumulation in CHO-K1 cells expressing human GPR119 at 10 µM concentration. Additionally, 5(S)-HEPE enhances glucose-stimulated insulin secretion from MING6 insulinoma pancreatic islets and glucagon-like peptide 1 (GLP-1) secretion from HuTu 80 adenocarcinoma cells at the same concentration. Notably, serum levels of 5(S)-HEPE are increased in hyperlipidemia patients.