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-P10341
    ZP3022
    		Agonist
    ZP3022 is a dual agonist of glucagon-like peptide-1 (GLP-1) and gastrin that has the ability to sustainably improve glycemic control. Additionally, ZP3022 can effectively increase β-cell mass, promote β-cell proliferation, and enhance the function of pancreatic islets. ZP3022 can be used in anti-diabetic research.
    ZP3022
  • HY-144134
    GLP-1R agonist 6
    		Agonist
    GLP-1R agonist 6 is a potent GLP-1R agonist with an EC50 of 0.15 nM for human GLP-1R (WO2021249492A1, compound 005A or 005B).
    GLP-1R agonist 6
  • HY-107129
    MK-3577
    		Antagonist
    MK-3577 is an orally effective glucagon receptor (GCGR) antagonist that reduces hepatic glucose production and lowers blood glucose levels by blocking glucagon receptors on target organs, primarily the liver. Pharmacokinetic analysis in domestic cats indicates that MK-3577 reaches peak levels 3 to 4 hours after oral administration, with a half-life of approximately 15 hours. MK-3577 can be used in diabetes research.
    MK-3577
  • HY-P2625S1
    GLP-2(3-33) (Leu-13C6,15NN) TFA
    		Agonist
    GLP-2(3-33) (Leu-13C6,15N) TFA is 13C and 15N labeled GLP-2(3-33) (HY-P2625). GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM).
    GLP-2(3-33) (Leu-<sup>13</sup>C<sub>6</sub>,<sup>15</sup>NN) TFA
  • HY-159696
    ISIS 449884
    		Inhibitor
    ISIS 449884 is a 2'-O-methoxyethyl antisense oligonucleotide that targets GCGR. ISIS 449884 has an ability to reduce hepatic glucose output and lower the blood glucose level. ISIS 449884 can be used for the study of type 2 diabetes mellitus (T2DM).
    ISIS 449884
  • HY-13443S
    Exendin-4 (Leu-13C6,15N) TFA
    Exendin-4 (Leu-13C6,15N) (Exenatide (Leu-13C6,15N)) TFA is the 13C- and 15N-labeled Exendin-4 TFA (HY-13443). Exendin-4 (Exenatide), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM.
    Exendin-4 (Leu-<sup>13</sup>C<sub>6</sub>,<sup>15</sup>N) TFA
  • HY-P3616
    Human glucagon-like peptide-1-(7-36)-Lys(Biotin) amide
    Human glucagon-like peptide-1-(7-36)-Lys(Biotin) amide is a biotin labeled glucagon-like peptide-1-(7-36). Glucagon-like peptide-1-(7-36) is a gastrointestinal peptide with antidiabetogenic activity, and can increase the release of insulin.
    Human glucagon-like peptide-1-(7-36)-Lys(Biotin) amide
  • HY-P3506B
    Retatrutide acetate
    		Agonist
    Retatrutide (LY3437943) acetate is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide acetate inhibits human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide acetate can be used for the research of obesity.
    Retatrutide acetate
  • HY-106559
    Sorbinicate
    		Inhibitor
    Sorbinicate, a derivative of nicotinic acid, exerts a favourable influence on blood rheology and platelet function.
    Sorbinicate
  • HY-P2880
    PHI-27 (porcine)
    PHI-27 (porcine) is a 27 amino acid peptide.PHI-27 (porcine) is used to find peptide hormones and other active peptides.
    PHI-27 (porcine)
  • HY-129656
    GLP-1 receptor agonist 3
    		Agonist
    GLP-1 receptor agonist 3 (compound (R)-4A-1) is a GLP-1 receptor agonist (WO2018109607A1), used for diabetes research. compound (S)-4A-1 shows EC50s of 1.1 nM and 13 nM in Clone H6 and Clone C6 cell lines assay, respectively.
    GLP-1 receptor agonist 3
  • HY-P0212
    Neuropeptide Y, porcine
    		Agonist
    Neuropeptide Y, porcine, a peptide in porcine brain, is capable of inhibiting secretin-stimulated pancreatic secretion.
    Neuropeptide Y, porcine
  • HY-144136
    GLP-1R agonist 8
    		Agonist
    GLP-1R agonist 8 is a potent GLP-1R agonist with an EC50 of < 2 nM (WO2021219019A1, compound 129a).
    GLP-1R agonist 8
  • HY-108795B
    [Gly8]-GLP-1(7-37) acetate
    		Agonist
    [Gly8]-GLP-1(7-37) (acetate) is a derivative of GLP-1 containing alanine-to-glycine substitution at positions 8. [Gly8]-GLP-1(7-37) (acetate) is also a peptide fragment of the GLP-1 receptor (GLP-1R) agonist Dulaglutide (HY-P0120).
    [Gly8]-GLP-1(7-37) acetate
  • HY-P4672
    (Met(O)27)-Glucagon (1-29) (human, rat, porcine)
    (Met(O)27)-Glucagon (1-29) (human, rat, porcine) is a modified glucagon. (Met(O)27)-Glucagon (1-29) (human, rat, porcine) has the same maximum glucose-synthesizing activity in rat hepatocytes as native glucagon, but it is less potent, suggesting a crucial role of methionine in the binding of glucagon to its hepatic receptor.
    (Met(O)27)-Glucagon (1-29) (human, rat, porcine)
  • HY-P5815
    GLP-1 (1-36) amide (human, rat)
    GLP-1 (1-36) amide (human, rat) (Glucagon-like Peptide 1 (1-36) amide (human, rat) ) is a molecular variant of glucagon-like peptide 1 (GLP-1)-(7-36) amide. GLP-1 (1-36) amide (human, rat) can stimulate [14C]aminopyrine accumulation on enzymatically dispersed enriched rat parietal cells.
    GLP-1 (1-36) amide (human, rat)
  • HY-P10736
    AMG133 peptide payload
    AMG133 peptide payload is a GLP-1 agonist that can be used as a peptide linker conjugate of Maridebart cafraglutide (AMG133) (HY-164535).
    AMG133 peptide payload
  • HY-P1144A
    Oxyntomodulin (bovine, porcine) (TFA)
    		Agonist
    Oxyntomodulin (bovine, porcine) TFA, a 37-amino acid peptide hormone, is a glucagon-like peptide 1 (GLP-1) receptor agonist.
    Oxyntomodulin (bovine, porcine) (TFA)
  • HY-153476
    GIP/GLP-1 dual receptor agonist-1
    		Agonist
    GIP/GLP-1 dual receptor agonist-1 (compound 4) is a GIP/GLP-1 receptor agonist. GIP/GLP-1 dual receptor agonist-1 can be used in the research of metabolic disorders and fatty liver diseases, including nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD).
    GIP/GLP-1 dual receptor agonist-1
  • HY-144033
    GLP-1R agonist 1
    		Agonist
    GLP-1R agonist 1 is a potent agonist of GLP-1R. GLP-1R agonist 1 is a thickened imidazole derivative compound. Glucagon-like peptide-1 (GLP-1) is an intestinal hypoglycemic hormone secreted by L-cells in the lower gastrointestinal tract. GLP-1R agonist 1 has the potential for the research of diabetes (extracted from patent WO2021197464A1, compound 4).
    GLP-1R agonist 1
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