GCGR Agonist

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.

Liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist used clinically to treat type 2 diabetes mellitus.

Orforglipron (LY3502970) (Compound 67) is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorates the type 2 diabete.

Retatrutide (LY3437943) is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide binds human GCGR, GIPR, and GLP-1R with EC₅₀ values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide can be used for the research of obesity.

Survodutide (BI 456906) sodium is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC₅₀s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide sodium, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide sodium has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake.

LY3324954 is a long-acting, highly selective glucagon receptor (GCGR) agonist. LY3324954 stimulates cAMP production via the hepatic GCGR signaling pathway and induces acute blood glucose elevation, while promoting FGF21 expression in the liver and plasma. LY3324954 reduces body weight and abdominal fat mass, increases energy expenditure, and effectively improves lipid homeostasis, insulin sensitivity, and glucose intolerance. LY3324954 can be used in obesity-related research.

Danuglipron (PF-06882961) is an orally active glucagon-like peptide-1 receptor (GLP-1R) agonist. Danuglipron has the potential for type 2 diabetes research.

Dulaglutide (LY2189265) is a glucagon-like peptide-1 (GLP-1) receptor agonist. Dulaglutide can be uesd for the research of type 2 diabetes (T2D) .

Mazdutide (IBI-362; LY-3305677) is a long-acting synthetic oxyntomodulin analog. Mazdutide is also a co-agonist of glucagon-like peptide (GLP-1R) and glucagon receptor (GCGR). Mazdutide binds human and mouse GCGR (K_i: 17.7 nM and 15.9 nM, respectively) and GLP-1R (K_i: 28.6 nM and 25.1 nM, respectively) and stimulates insulin secretion from mouse islets (EC₅₀: 5.2 nM). Mazdutide is used in studies of obesity and type 2 diabetes (T2D).

Survodutide (BI 456906) is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC₅₀s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake.

GLP-1R agonist 2 (compound 2) is an effective GLP-1R agonist that exerts its activating effect by forming hydrogen bonds with the Tyr42, Cys71, and Ser84 residues of GLP-1R. GLP-1R agonist 2 has the potential for research in metabolic diseases such as type 2 diabetes and obesity.

GLP-1(7-36), amide is a physiological incretin hormone that stimulates insulin secretion.

Zenagamtide (Amycretin; NN 9487) sodium is an orally active, blood-brain barrier permeable triple agonist that targets GLP-1, amylin (Amylin Receptor) and calcitonin receptor (Calcitonin Receptor). Zenagamtide sodium is a single peptide consisting of 68 amino acids that can target brain regions regulating food intake, significantly suppress appetite and reduce energy intake. Therefore, Zenagamtide sodium improves body weight, waist circumference, glycated hemoglobin and lipid profile, and also alleviates the histological features of metabolic dysfunction-associated steatotic liver disease (MASLD) and enhances insulin sensitivity. Zenagamtide sodium may cause transient increases in heart rate and fluctuations in serum calcium levels, but it is an important compound for the study of overweight, obesity, insulin resistance and related metabolic diseases.

Retatrutide (LY3437943) TFA is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide TFA binds human GCGR, GIPR, and GLP-1R with EC₅₀ values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide TFA can be used for the research of obesity.

BETP is an agonist of glucagon-like peptide-1 (GLP-1) receptor, with EC₅₀s of 0.66 and 0.755 μM for human and rat GLP-1 receptor, respectively.

GLP-2(1-33) (human) is an enteroendocrine hormone which can bind to the GLP-2 receptor and stimulate the growth of intestinal epithelium.

AMG133 peptide payload TFA is a GLP-1 analog agonist peptide. AMG133 peptide payload TFA potently activates GLP-1R and exhibits weight loss and metabolic improvement activities. AMG133 peptide payload TFA can be used for the synthesis of AMG 133 (HY-164535).

Exendin-4 acetate (Exenatide acetate), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC₅₀ of 3.22 nM.

Orforglipron hemicalcium hydrate (LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate) is the calcium salt hydrate form of Orforglipron (HY-112185). Orforglipron is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorating the type 2 diabete.

Bay 55-9837 is a potent and highly selective agonist of VPAC2, with a K_d of 0.65 nM. Bay 55-9837 may be a useful therapy for the research of type 2 diabetes.