1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. GPR119

GPR119

G Protein-Coupled Receptor 119

G protein-coupled receptor 119 (GPR119) is a member of the class A (rhodopsin-type) GPCR family, which is highly expressed on only a limited number of tissues, such as pancreatic β-cells and enteroendocrine cells of the gastrointestinal tract in humans. The activation of GPR119 has the stimulatory effects of glucose-dependent insulin secretion in pancreatic β-cells as well as intestinal secretion of incretin hormones including glucose-dependent insulinotropic peptide (GIP) and glucagon-likepeptide1 (GLP-1). Taken together, these effects represented a potential mechanism for modulation of glucose homeostasis and an attractive approach to the treatment of type 2 diabetes mellitus (T2DM). GPR119 can be activated by oleoylethanolamide and several other endogenous lipids containing oleic acid: these include N-oleoyl-dopamine, 1-oleoyl-lysophosphatidylcholine, generated in the tissue, and 2-oleoyl glycerol generated in the gut lumen.

GPR119 Related Products (13):

Cat. No. Product Name Effect Purity
  • HY-15291
    MBX-2982
    Agonist 98.51%
    MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.
  • HY-12066
    GSK1292263
    Agonist 99.71%
    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).
  • HY-107535
    AS1269574
    Agonist 98.76%
    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.
  • HY-15565
    APD668
    Agonist 99.10%
    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 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes.
  • HY-15564
    AR 231453
    Agonist 99.84%
    AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s.
  • HY-146468
    DPP-4/GPR119 modulator 1
    Agonist
    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.
  • HY-146469
    DPP-4/GPR119 modulator 2
    Agonist
    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.
  • HY-15566
    APD597
    Agonist 99.97%
    APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119.
  • HY-108258
    PSN 375963
    Agonist 99.96%
    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).
  • HY-W011121
    2-Oleoylglycerol
    Agonist ≥98.0%
    2-Oleoylglycerol is a dietary naturally occurring lipid. 2-Oleoylglycerol is a GPR119 agonist, with an EC50 of 2.5 μM for human GPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol stimulates glucagon-like peptide-1 (GLP-1) secretion in vivo.
  • HY-16673
    PSN632408
    Agonist 99.64%
    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.
  • HY-109032
    Firuglipel
    Agonist 99.21%
    Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.
  • HY-108258A
    PSN 375963 hydrochloride
    Agonist
    PSN 375963 hydrochloride is a potent GPR119 agonist, with EC50s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 hydrochloride shows similar potency to the endogenous agonist oleoylethanolamide (OEA).