2. Signaling Pathways
  3. GPCR/G Protein
  4. GCGR

GCGR

Glucagon Receptor

GCGR

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GCGR (glucagon receptor) is in the G protein-coupled receptor family, that is important in controlling blood glucose levels. The glucagon receptor is a 62 kDa protein that is activated by glucagon and is a member of the class B G-protein coupled family of receptors, coupled to G alpha i, Gs and to a lesser extent G alpha q. Stimulation of the receptor results in activation of adenylate cyclase and increased levels of intracellular cAMP. In humans, the glucagon receptor is encoded by the GCGR gene. Glucagon receptors are mainly expressed in liver and in kidney with lesser amounts found in heart, adipose tissue, spleen, thymus, adrenal glands, pancreas, cerebral cortex, and gastrointestinal tract.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P3050
    Helospectin II
    		Inhibitor
    Helospectin II is a neuropeptide of the vasoactive intestinal peptide (VIP) family. Helospectin II has vasodilatory and antihypertensive activities, and decreases blood pressure. Helospectin II is originally isolated from the salivary gland venom of the lizard Heloderma suspectum.
    Helospectin II
  • HY-P3621
    Biotinyl-Glucagon (1-29), human, bovine, porcine
    Biotinyl-Glucagon (1-29), human, bovine, porcine is a biotinylated glucagon. Glucagon is a peptide hormone, produced by α-cells of the pancreas, can increase concentration of glucose and fatty acids in the bloodstream.
    Biotinyl-Glucagon (1-29), human, bovine, porcine
  • HY-P11487
    UTG-4
    		Agonist
    UTG-4 is a GLP-1R, GIPR, and GCGR agonist with EC50 values of 126.3 pM, 29.2 pM, and 250.2 pM, respectively. UTG-4 binds to HSA (Kd = 14.6 μM). UTG-4 effectively alleviates endothelial-mesenchymal transition. UTG-4 promotes weight loss, inhibits food intake, improves glucose tolerance, and has a significant anti-atherosclerotic effect.
    UTG-4
  • HY-129657
    GLP-1 receptor agonist 4
    		Agonist
    GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist extracted from patent WO2009111700A2, compound 87, has an EC50 of 64.5 nM. GLP-1 receptor agonist 4 can be used in the research for treatment of diabetes.
    GLP-1 receptor agonist 4
  • HY-172836S
    GLP-1 receptor agonist 17-d3
    		Agonist
    GLP-1 receptor agonist 17-d3 (Compound 701) is the deuterium labeled GLP-1R agonist 17 (HY-148212). GLP-1R agonist 17 is a GLP-1 receptor agonist that can be used for the research of cardiovascular metabolic diseases.
    GLP-1 receptor agonist 17-d<sub>3</sub>
  • HY-P11279
    TC2
    		Agonist
    TC2 is an efficient GIPR-preferring monomeric quadruple agonist that can respectively activate GIPR, GLP-1R, GcgR, and Y2R with IC50 values of 0.47, 2.1, 30, and 55 nM respectively. TC2 exhibits a significant GLP-1R preference, with a significant reduction in β-inhibitory protein 2 (βArr2) recruitment, while maintaining a strong cAMP signal. TC2 can be used for research on obesity and diabetes.
    TC2
  • HY-13443F
    Exendin 4, biotin labeled
    		Agonist
    Exendin 4, biotin labeled is a biotin labeled Exendin 4 (HY-13443). Exendin 4 is a long-acting GLP-1 receptor agonist.
    Exendin 4, biotin labeled
  • HY-P3101A
    GLP-1(28-36)amide TFA
    GLP-1(28-36)amide TFA, a C-terminal nonapeptide of GLP-1, is a major product derived from the cleavage of GLP-1 by the neutral endopeptidase (NEP). GLP-1(28-36)amide TFA is an antioxidant and targets to mitochondrion, inhibits mitochondrial permeability transition (MPT). GLP-1(28-36)amide TFA has anti-diabetic and cardioprotection effects.
    GLP-1(28-36)amide TFA
  • HY-169707
    GCGR antagonist 3
    		Antagonist
    GCGR antagonist 3 (example 1) is an antagonist of the glucagon receptor (GCGR) and can be used in diabetes research.
    GCGR antagonist 3
  • HY-P992007
    PF-06293620
    		Antagonist
    PF-06293620 (RN909) is a monoclonal antibody antagonist of the glucagon receptor. PF-06293620 produces dose-dependent, durable lowering of fasting plasma glucose and reduces HbA1c levels. PF-06293620 can be used for the research of type 2 diabetes mellitus.
    PF-06293620
  • HY-P10337
    OXM-7
    		Agonist
    OXM-7 is a dual agonist of GLP-1R (EC50=0.024 nM) and GCGR (EC50=0.082 nM). OXM-7 can enhance glucose-stimulated insulin secretion and hepatic glucose output. OXM-7 lowers blood glucose levels. OXM-7 improves lipid metabolism.
    OXM-7
  • HY-12525B
    LGD 6972 ammonium
    		Antagonist
    LGD-6972 ammonium is a selective and orally active glucagon receptor antagonist. LGD-6972 ammonium has the potential for type 2 diabetes research.
    LGD 6972 ammonium
  • HY-P3608
    [Des-His1,Glu9] Glucagon
    		Antagonist
    [Des-His1,Glu9] Glucagon is a potent glucagon receptor system peptide antagonist. [Des-His1,Glu9] Glucagon enhances the glucose-stimulated release of insulin from pancreatic islet cells. [Des-His1,Glu9] Glucagon can be used to research diabetes.
    [Des-His1,Glu9] Glucagon
  • HY-P5578A
    A8SGLP-1 TFA
    		Agonist
    A8SGLP-1 TFA is an orally active GLP-1 analogue that the alanine at position 8 substituted with serine. A8SGLP-1 TFA reduces blood glucose in db/db mice without affecting its function.
    A8SGLP-1 TFA
  • HY-171851
    GLP-1R agonist 32
    		Agonist
    GLP-1R agonist 32 (Compound 111) is an orally active and highly potent GLP-1R agonist with an EC50 value of 0.017 nM. GLP-1R agonist 32 exerts glucose-regulating activity by activating GLP-1R to stimulate cAMP production, promoting insulin secretion, inhibiting glucagon release, and delaying gastric emptying. GLP-1R agonist 32 is promising for research of type 2 diabetes, obesity, and related metabolic disorders.
    GLP-1R agonist 32
  • HY-181709
    TPM003
    		Agonist
    TPM003 (TG062) is a triple agonist of GLP-1R, GIPR and GCGR, with EC50 values of 33.9, 12.5 and 92.9 pM, respectively. TPM003 suppresses appetite, regulates blood glucose, enhances insulin sensitivity, reduces gastrointestinal intolerance, promotes hepatic lipid mobilization and increases energy expenditure. TPM003 induces weight loss, improves metabolic parameters, reverses hepatic steatosis and optimizes liver function markers. TPM003 is applicable for research on obesity and non-alcoholic steatohepatitis.
    TPM003
  • HY-P0211
    [Ac-Tyr1,D-Phe2]GRF 1-29, amide (human)
    		Antagonist
    [Ac-Tyr1,D-Phe2]GRF 1-29, amide (human), a growth hormone releasing factor (GRF) analogue, is a vasoactive intestinal peptide (VIP) antagonist.
    [Ac-Tyr1,D-Phe2]GRF 1-29, amide (human)
  • HY-N0630R
    Shanzhiside methyl ester (Standard)
    		Agonist
    Shanzhiside methyl ester (Standard) is the analytical standard of Shanzhiside methyl ester. This product is intended for research and analytical applications. Shanzhiside methy lester is isolated from lamiophlomis rotata. Shanzhiside methyl ester is a small molecule glucagon-like peptide-1 (GLP-1) receptor agonist and has the ability to induce anti-allodynic tolerance.
    Shanzhiside methyl ester (Standard)
  • HY-180444
    Glucagon receptor antagonist-9
    		Antagonist
    Glucagon receptor antagonist-9 (compound 13) is a potent glucagon receptor antagonist with a pIC50 of 7.000.
    Glucagon receptor antagonist-9
  • HY-103547R
    L-168049 (Standard)
    		Antagonist
    L-168049 (Standard) is the analytical standard of L-168049 (HY-103547). This product is intended for research and analytical applications. L-168049 is a potent, selective, orally active and non-competitive glucagon receptor antagonist with IC50s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine glucagon receptors, respectively.
    L-168049 (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity