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

GPR119

G Protein-Coupled Receptor 119

GPR119

Related Products

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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 (39):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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. 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.
    DPP-4/GPR119 modulator 2
  • HY-178780
    MKP10241
    		Agonist 98.06%
    MKP10241 is an orally active GPR119 agonist. MKP10241 elevates cAMP levels in the GPR119 expressing cell line (EC50: 3.7 nM). MKP10241 reduces blood glucose levels and HbA1c in acute models and a chronic diabetic mouse model. MKP10241 also demonstrates excellent preclinical efficacy in acute as well as chronic rodent models of obesity, and MASH.
    MKP10241
  • HY-124978
    MK-8282
    		Agonist
    MK-8282 is a potent, orally active GPR-119 agonist. MK-8282 shows improved glucose tolerance. MK-8282 can be used in the research of type 2 diabetes.
    MK-8282
  • HY-182454
    GPR119 agonist 4
    		Agonist
    GPR119 agonist 4 is a GPR119 agonist and oral glucose-lowering agent with a human GPR119 EC50 of 42 nM.GPR119 agonist 4 activates GPR119.GPR119 agonist 4 reduces blood glucose area under the curve in an oral glucose tolerance test.GPR119 agonist 4 exhibits improved clearance in liver microsomes.GPR119 agonist 4 can be used for the research of type 2 diabetes mellitus.
    GPR119 agonist 4
  • 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).
    PSN 375963 hydrochloride
  • HY-W701772
    2-Oleoylglycerol-d5
    2-Oleoylglycerol-d5 (2-OG-d5) is the deuterium labeled 2-Oleoylglycerol (HY-W011121). 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) .
    2-Oleoylglycerol-d<sub>5</sub>
  • HY-12375
    BMS-903452
    		Agonist
    BMS-903452 is a potent and selective GPR119 agonist for diabetes research.
    BMS-903452
  • HY-113653
    GSK2041706A
    		Agonist
    GSK2041706A (GSK706) is a potent G protein-coupled receptor 119 (GPR119) agonist. GSK2041706A can be used for the research of type 2 diabetes.
    GSK2041706A
  • HY-12066A
    GSK-1292263 hydrochloride
    		Agonist
    GSK-1292263 (hydrochloride) is an orally active GPR119 agonist (pEC50 of approximately 6.9 and 6.7 nM for human and rat GPR119, respectively). GSK-1292263 is used in the research of type 2 diabetes and dyslipidemia.
    GSK-1292263 hydrochloride
  • HY-155553
    GPR119 agonist 2
    		Agonist
    GPR119 agonist 2 (compound 43) is an orally active GPR119 agonist. GPR119 agonist 2 shows good pharmacokinetic characteristics in rodents and can effectively improve glucose tolerance in mice and rats. GPR119 agonist 2 has the potential to study type 2 diabetes.
    GPR119 agonist 2
  • HY-108258R
    PSN 375963 (Standard)
    		Agonist
    PSN 375963 (Standard) is the analytical standard of PSN 375963 (HY-108258). This product is intended for research and analytical applications. 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).
    PSN 375963 (Standard)
  • HY-15291R
    MBX-2982 (Standard)
    		Agonist
    MBX-2982 (Standard) is the analytical standard of MBX-2982. This product is intended for research and analytical applications. MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.
    MBX-2982 (Standard)
  • HY-107535R
    AS1269574 (Standard)
    		Agonist
    AS1269574 (Standard) is the analytical standard of AS1269574 (HY-107535). This product is intended for research and analytical applications. 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.
    AS1269574 (Standard)
  • HY-15564R
    AR 231453 (Standard)
    		Agonist
    AR 231453 (Standard) is the analytical standard of AR 231453. This product is intended for research and analytical applications. AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s.
    AR 231453 (Standard)
  • HY-15565R
    APD668 (Standard)
    		Agonist
    APD668 (Standard) is the analytical standard of APD668. This product is intended for research and analytical applications. 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.
    APD668 (Standard)
  • HY-117446A
    AS-1669058 free base
    		Agonist
    AS-1669058 free base is a GPR119 agonist and a potential inhibitor of type 2 diabetes. AS-1669058 free base induces insulin secretion induced by high blood glucose levels in vitro and in vivo and increases insulin promoter activity. In animal studies, AS-1669058 free base improved glucose tolerance and reduced blood glucose levels in db/db mice.
    AS-1669058 free base
  • HY-117446
    AS-1669058
    		Agonist
    AS-1669058 is a GPR119 agonist and a potential inhibitor of type 2 diabetes. AS-1669058 induces insulin secretion in response to high blood glucose levels in vitro and in vivo and increases insulin promoter activity. In animal studies, AS-1669058 improved glucose tolerance and reduced blood glucose levels in db/db mice.
    AS-1669058
  • HY-109032R
    Firuglipel (Standard)
    		Agonist
    Firuglipel (Standard) is the analytical standard of Firuglipel (HY-109032). This product is intended for research and analytical applications. Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.
    Firuglipel (Standard)
  • HY-12066R
    GSK1292263 (Standard)
    		Agonist
    GSK1292263 (Standard) is the analytical standard of GSK1292263. This product is intended for research and analytical applications. 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).
    GSK1292263 (Standard)