gpr119

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).

DPP-4/GPR119 modulator 1 (Compound 22) is an orally active compound that functions as both a dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist. It demonstrates a glucose-lowering effect in blood and exhibits moderate inhibition of the hERG channel, with an IC50 value of 4.9 µM. This compound is applicable in diabetes research [1].

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].

AR 231453 is a selective and orally available GPR119 agonist,can stimulate β-cell replication and improve islet graft function.

BMS-903452 is a potent and selective GPR119 agonist with EC50 of 14 nM. BMS-903452 is indicated for the treatment of acute and chronic rodent diabetes. GPR119 was mainly expressed in pancreatic b cells and gastrointestinal endocrine cells. GPR119 had no significant inhibitory effect on 9 different cytochrome P450 enzymes (IC50 > 40 μM), did not activate PXR (EC50>50 μM), and was not toxic to liver (HEPG2) cell lines.

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

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.

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

PSN632408 is an optimized agonist of GPR119 receptors that display similar potency to OEA at both recombinant mouse and human GPR119 receptors (EC50: 5.6 and 7.9 uM, respectively).

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

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

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.

Firuglipel is an orally available and selective agonist of GPR119.

GSK706 is a novel effective agonist of the GPR119.

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].

AS1269574 is a potent, orally available GPR119 agonist. AS1269574(AS 1269574) has the potential for the research 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.

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

GSK1104252A is a potent and selective agonist of GPR119.

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

BMS-986034 is a GPR119 agonist.

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

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.

AS1907417 is a GPR119 agonist.

Tirzepatide sodium salt (LY3298176 sodium salt) is a GIP and GLP-1 receptor agonist with neuroprotective activity and can be used to treat obesity.

Tirzepatide (LY-3298176) is a dual agonist of glucose-dependent polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor with neuroprotective activity for the study of diabetes and obesity.

Tirzepatide acetate is a dual GIP / GLP-1 receptor agonist.