gpr119

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

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

Firuglipel is an orally available and selective agonist of GPR119.

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

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.

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

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

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.

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

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 acts as both a dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist, demonstrating a glucose-lowering effect in blood and 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].

MKP10241 is an orally bioavailable GPR119 agonist that increases cAMP levels in GPR119-expressing cell lines with an EC₅₀ of 3.7 nM. It significantly reduces blood glucose and glycated hemoglobin (HbA1c) levels in acute and chronic diabetic mouse models. It also exhibits favorable pharmacological activities in acute and chronic obesity models and MASH rodent models.

PSN632408 is a selective GPR119 agonist that is orally active and exhibits agonist potency comparable to that of OEA in mouse and human receptors. PSN632408 modulates pancreatic β-cell function in vitro and in animal models and may improve metabolic parameters, making it suitable for mechanistic studies of obesity and related metabolic disorders.

YH18968, a GPR119 agonist, improves glucose tolerance and enhances blood glucose-lowering effects. When combined with dipeptidyl peptidase-4 (DPP-4) inhibitors, YH18968 increases the plasma levels of active GLP-1 in normal mice.

DA-1241 is a GPR119 agonist. By activating GPR119, it downregulates NFκB signaling, thereby inhibiting macrophage differentiation. Whether used alone or in combination with DPP4 inhibitors, DA-1241 can alleviate liver inflammation and restore the expression of liver genes linked to inflammation. It is applicable in the research of metabolic dysfunction-associated steatohepatitis (MASH).

GSK-1292263 (hydrochloride) is an orally active GPR119 agonist with a pEC50 of approximately 6.9 nM for human and 6.7 nM for rat GPR119. It is utilized in research related to type 2 diabetes and dyslipidemia.

K-833 is a GPR119 agonist with EC50 values of 39.8 nM, 100 nM, 75.4 nM, and 12.6 nM for human, mouse, rat, and dog respectively. In acute intestinal peptide secretion in mice, K-833 modestly increases the secretion of glucagon-like peptide-1 (GLP-1) and, when used in combination with AM-5262, can synergistically enhance GLP-1 levels. K-833 is applicable in weight loss 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].

GSK706 is a novel effective agonist of the GPR119.

AS1907417 is a GPR119 agonist.

GSK1104252A is a potent and selective agonist of GPR119.