GPR119 Agonist

2-Oleoylglycerol (2-OG) is a lipid found in the diet. It is a GPR119 agonist, with an EC₅₀ value of 2.5 μM in activating hGPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol enhances the inflammatory response of macrophages and promotes fibrosis by activating the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. It also stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. 2-Oleoylglycerol is expected to be used in the research of non-alcoholic steatohepatitis (NASH) .

MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.

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

GSK-1292263 is an orally available GPR119 agonist with pEC₅₀s of 6.9 and 6.7 for human and rat GPR119, respectively. GSK-1292263 can be used for the research of type 2 diabetes mellitus (T2DM).

APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC₅₀s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (K_i=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes.

HBK001 is an orally active and selective dual GPR119 agonist and DPP-IV inhibitor. HBK001 triggers cAMP production, PKA activation, CREB phosphorylation, glucose-stimulated insulin secretion, plasma incretin elevation, β-cell proliferation, and β-cell function gene up-regulation. HBK001 reduces blood glucose, ameliorates hyperglycemia, improves glucose tolerance, and enhances islet morphology. HBK001 can be used for the research of type 2 diabetes mellitus.

AZ13581837 is an orally active GPR120 agonist with an EC₅₀ of 5.2 nM for human GPR120. AZ13581837 signals through Gαq, Gαs, and β-arrestin pathways, reduces cAMP production, stimulates GLP-1 secretion, induces glucose lowering, and increases insulin secretion. AZ13581837 can be used for the research of type 2 diabetes.

APD597 (JNJ-38431055) is an orally active agonist of GPR119. APD597 exhibits reduced CYP2C9 inhibition with an IC₅₀ of 5.8 μM. APD597 can be studied in research for type 2 diabetes.

Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.

DA-1241 is a GPR119 agonist. DA-1241 reduces macrophage differentiation through downregulation of NFκB signaling by activating GPR119. DA-1241, alone and in combination with a DPP4 inhibitor, reduces liver inflammation and restores inflammation-related liver gene expression. DA-1241 can be used for the research of metabolic dysfunction-associated steatohepatitis (MASH).

AS1269574 is a potent, orally available GPR119 agonist, with an EC₅₀ of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates TRPA1 cation channels to stimulate glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induces glucose-dependent insulin secretion from pancreatic β-cells only under high-glucose conditions. AS1269574 has the potential for the research of type 2 diabetes.

PSN632408, a selective, orally active GPR119 agonist, shows similar potency to OEA at both recombinant mouse and human GPR119 receptors (EC₅₀=5.6 and 7.9 uM, respectively). PSN632408 can stimulate β-cell replication and improve islet graft function. PSN632408 has the potential for the research of obesity and related metabolic disorders.

PSN 375963 is a potent GPR119 agonist, with EC₅₀s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 shows similar potency to the endogenous agonist oleoylethanolamide (OEA).

BMS-903452 is a potent and selective GPR119 agonist for diabetes research.

DPP-4/GPR119 modulator 1 (Compound 22) is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist. DPP-4/GPR119 modulator 1 shows blood glucose-lowering effect and moderate inhibition on hERG channel with an IC₅₀ of 4.9 μM. DPP-4/GPR119 modulator 1 can be used for diabetes research. DPP-4/GPR119 modulator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

GPR119 agonist 3 (Compound 21b) is an orally active agonist of GPR119 with an EC₅₀ value of 3.8 nM for hGPR119. Additionally, GPR119 agonist 3 exhibits hypoglycemic effects and can be used in research on type 2 diabetes and obesity.

K-833 is a GPR119 agonist with EC₅₀ values of 39.8 nM (human), 100nM (mouse), 75.4 nM (rat) and 12.6 nM (dog). K-833 demonstrates a modest increase in GLP-1 secretion and leads to a synergistic increase in GLP-1 levels when combined with AM-5262 (HY-16619) in acute gut peptide secretion assays in mice. K-833 can be used in studies on weight loss.

BMS-986034 is an orally active ingredient (API) that is an agonist of GPR119..

AS1907417 is a novel GPR119 agonist with an oral activity. AS1907417 is a modified form of AS1269574. AS1907417 has antihyperglycemic and can be used in the research of type 2 diabetes.

DPP-4/GPR119 modulator 2 (Compound 20i) is a dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist with an IC₅₀ of 0.22 μM for DPP-IV and an EC₅₀ of 0.95 μM for GPR119. DPP-4/GPR119 modulator 2 can be used for diabetes research. DPP-4/GPR119 modulator 2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.