GCGR Antagonist

MK 0893 is a potent and selective glucagon receptor antagonist with an IC₅₀ of 6.6 nM.

GLP-1(9-36)amide is a major metabolite of glucagon-like peptide-1-(7-36) amide formed by the enzyme dipeptidyl peptidase-4 (DPP-4). GLP-1(9-36)amide acts as an antagonist to the human pancreatic GLP-1 receptor.

GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC₅₀ of 650 nM.

Adomeglivant (LY2409021) is a potent, selective glucagon receptor (GluR) allosteric antagonist. Adomeglivant is widely used in the research for type 2 diabetes mellitus.

VIP(6-28)(human, rat, porcine, bovine) is an effective antagonist of the actions of exogenous vasoactive intestinal peptide (VIP) on cAMP.

LGD-6972 is a selective and orally active glucagon receptor antagonist. LGD-6972 has the potential for type 2 diabetes research.

Volagidemab is an antagonistic glucagon receptor (GCGR) monoclonal antibody (mAb). Volagidemab can be used in the research of type 1 diabetes (T1D).

PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist. PF-06291874 is under the study for type 2 diabetes mellitus (T2DM).

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.

GLP-1(9-36)amide TFA is a major metabolite of glucagon-like peptide-1-(7-36) amide formed by the enzyme dipeptidyl peptidase-4 (DPP-4). GLP-1(9-36)amide TFA acts as an antagonist to the human pancreatic GLP-1 receptor.

[Des-His1,Glu9]-Glucagon amide TFA is a potent and peptide antagonist of the glucagon receptor, with a pA₂ of 7.2. [Des-His1,Glu9]-Glucagon amide TFA is potentially useful in the study of the pathogenesis of diabetes.

Glucagon receptor antagonist-3 is a highly potent glucagon receptor antagonist.

Glucagon receptor antagonist-2 is a glucagon receptor antagonist. Glucagon receptor antagonist-2 functionally inhibits receptor activity via reduced cAMP production. Glucagon receptor antagonist-2 can be used for the research of type 2 diabetes.

NNC 92-1687 is a non-peptide competitive human glucagon receptor antagonist (IC₅₀=20 μM; K_i=9.1 μM). NNC 92-1687 can be used in the research of type 2 diabetes.

Pemvidutide (ALT-801) TFA is a GLP-1R/GCGR dual agonist, shows striking reductions in body weight, liver fat and serum lipids. Pemvidutide TFA can be used in non-alcoholic steatohepatitis (NASH) and obesity research.

GCGR antagonist 2, a Furan-2-carbohydrazide, is an orally active glucagon receptor antagonist. GCGR antagonist 2 binds to hGluR with an K_d value of 2.3 nM, and inhibits rat receptor with an IC₅₀ value of 0.43 nM. GCGR antagonist 2 inhibits glucagon-stimulated glycogenolysis.

Skyrin is an anthraquinone compound that can be isolated from almond fruit. Skyrin is a receptor-selective glucagon antagonist. Skyrin can inhibit the growth of tumor cells.

Exendin-3 is a biologically active peptides isolated from venoms of the Gila monster lizards, Heloderma horridurn.

Exendin (5-39) is a potent glucagon-like peptide 1 (GLP-1) receptor antagonist. Exendin (5-39) improves memory impairment in β-amyloid protein-treated rats.

[Des-His1,Glu9]-Glucagon amide is a potent and peptide antagonist of the glucagon receptor, with a pA₂ of 7.2. [Des-His1,Glu9]-Glucagon amide is potentially useful in the study of the pathogenesis of diabetes.