gpr119 agonist 2

GPR119 agonist 2 (compound 43), an orally active agonist of GPR119, exhibits favorable pharmacokinetic properties in rodents and has demonstrated efficacy in enhancing glucose tolerance in both mice and rats, indicating its potential in type 2 diabetes research [1].

GPR119 agonist3 (Compound 21b) is an orally active GPR119 agonist with an EC50 value of 3.8 nM for hGPR119. It also exhibits glucose-lowering effects and is applicable in research related to type 2 diabetes and obesity.

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

PSN 375963 hydrochloride, a potent GPR119 agonist, demonstrates EC50 values of 8.4 μM and 7.9 μM for human and mouse GPR119, respectively. Its efficacy is comparable to that of the endogenous agonist oleoylethanolamide (OEA) [1] [2].

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.

Selective medium-chain free fatty acid receptor GPR84 agonist (EC50 = 139 nM). Exhibits no response at GPR40, GPR41, GPR119 or GPR120 at 100 μM. Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK1 2 phosphorylation, receptor desensitization and internalization in vitro. Liu et al (2016) Design and synthesis of 2-alkylpyrimidine-4,6-diol and 6-alkylpyridine-2,4-diol as potent GPR84 agonists. ACS Med.Chem.Lett. 7 579 PMID:27326330 |Zhang et al (2016) Discovery and characterization of a novel small-molecule agonist for medium-chain free fatty acid receptor G protein-coupled receptor 84. J.Pharmacol.Exp.Ther. 357 337 PMID:26962172

2-Oleoylglycerol is a lipid found in palm kernel, sunflower seed and rice bran.2-Oleoylglycerol acts as a GPR119 agonist with neuroprotective effects and induces secretion of glucagon-like peptide 1 (GLP-1).2-Oleoylglycerol is used in the modelling of non-alcoholic steatohepatitis.

DPP-4 GPR119 modulator 2 is an inhibitor of dipeptidyl peptidase IV (DPP-IV) (IC50: 0.22 μM) and an agonist of GPR119 (EC50: 0.95 μM).

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

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.