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

GCGR

Glucagon Receptor

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-P5161
    FC382K10W15
    Agonist
    FC382K10W15 is a glucagon analogue and GLP-1R/GCGR agonist. FC382K10W15 can be used in type 2 diabetes research.
    FC382K10W15
  • HY-P5578
    A8SGLP-1
    Agonist
    A8SGLP-1 is an orally active GLP-1 analogue that the alanine at position 8 substituted with serine. A8SGLP-1 reduces blood glucose in db/db mice without affecting its function.
    A8SGLP-1
  • HY-P11044
    GEP12
    Agonist
    GEP12 is a GLP-1R/Y1-R/Y2-R tri-receptor agonist peptide with an EC50 of 17.3 nM and an IC50 of 19.2 nM for receptor binding. GEP12 may promote glycemic control and weight loss.
    GEP12
  • HY-P0212A
    Neuropeptide Y, porcine TFA
    Neuropeptide Y, porcine TFA, a peptide in porcine brain, is capable of inhibiting secretin-stimulated pancreatic secretion.
    Neuropeptide Y, porcine TFA
  • HY-144135
    GLP-1R agonist 7
    Agonist
    GLP-1R agonist 7 is a potent GLP-1R agonist with an EC50 of 0.67 µM (WO2021244645A1, compound WXA001).
    GLP-1R agonist 7
  • HY-P3542
    Des His1, Glu8 Exendin-4
    Antagonist
    Des His1, Glu8 Exendin-4 is a potent glucagon-like peptide-1 receptor (GLP-1-R) antagonist. Des His1, Glu8 Exendin-4 improves glucose homeostasis by regulating both insulin secretion and glucose production. Des His1, Glu8 Exendin-4 can be used for the research of type 2 diabetic and gastrointestinal.
    Des His1, Glu8 Exendin-4
  • HY-P5161A
    FC382K10W15 TFA
    Agonist
    FC382K10W15 TFA is a glucagon analogue and GLP-1R/GCGR agonist. FC382K10W15 TFA can be used in type 2 diabetes research.
    FC382K10W15 TFA
  • HY-P3539
    Exendin-4 (3-39)
    Exendin-4 (3-39) is a peptide. Exendin-4 (3-39) is a truncated form of Exendin-4 (HY-13443) that lacks the first two amino acids. Exendin-4 is a potent Glucagon-like peptide-1 receptor (GLP-1r) agonist. Exendin-4 (3-39) and Exendin-4 can be used for the research of diabetic and hypothalamic-pituitary-adrenal (HPA) axis.
    Exendin-4 (3-39)
  • HY-P4503
    (D-His1)-Exenatide
    Control
    (D-His1)-Exenatide is one od impurities of Exenatide.
    (D-His1)-Exenatide
  • HY-120401
    Glybuzole
    Activator
    Glybuzole (Desaglybuzole) is an orally active hypoglycaemic agent that has antidiabetic effect.
    Glybuzole
  • 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-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-P11275
    TC4
    Agonist
    TC4 is a highly balanced single-molecule quadruple agonist that can respectively activate GIPR, GLP-1R, GcgR, and Y2R with IC50 values of 0.95, 31, 81, and 1100 nM respectively. TC4 exhibits extremely strong signal bias on GLP-1R and has very low recruitment efficacy for β-inhibitor protein 2 (βArr2) and this strong cAMP preference is believed to maximize metabolic benefits (such as weight loss and hypoglycemia) while possibly minimizing side effects mediated by β-inhibitor protein recruitment (such as receptor desensitization). TC4 can be used for research on obesity and diabetes.
    TC4
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity