GCGR Agonist

Dapiglutide (ZP7570) is a long-acting glucagon-like peptide-1 receptor 1R (GLP-1R)/Glucagon-like peptide-2 receptor (GLP-2R) dual agonist. Dapiglutide alleviates intestinal dysfunction in a mouse short bowel model and has anti-obesity effects.

Cotadutide (MEDI0382) is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and GCGR with EC₅₀ values of 6.9 pM and 10.2 pM, respectively. Cotadutide exhibits ability to facilitate both weight loss and glycaemic control, and alleviate fibrosis. Cotadutide can be used in the research of obesity and type 2 diabetes (T2D).

Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist developed for treatment of type 2 diabetes, with an EC₅₀ value of 0.06 nM.

GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC₅₀=5.8 nM).

Glepaglutide (ZP1848) acetate, a long-acting GLP-2 analogue, is a potent GLP-2R agonist. Glepaglutide acetate reduces faecal output and increases intestinal absorption. Glepaglutide acetate alleviates small intestinal inflammation. Glepaglutide acetate can be used in the research of inflammatory bowel disease (IBD) and Crohn’s disease.

Liraglutide-¹³C₆,¹⁵ tetraTFA is the ¹³C and ¹⁵N labeled Liraglutide (HY-P0014). Liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist used for the study of type 2 diabetes mellitus.

Oxyntomodulin (bovine, porcine), a 37-amino acid peptide hormone, is a glucagon-like peptide 1 (GLP-1) receptor agonist.

Glucagon-like peptide 1 (1-37), human (TFA) is a highly potent agonist of the GLP-1 receptor.

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

Survodutide (BI 456906) TFA 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 TFA, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide TFA has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake.

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.

Glepaglutide (ZP1848), a long-acting GLP-2 analogue, is a potent GLP-2R agonist. Glepaglutide reduces faecal output and increases intestinal absorption. Glepaglutide alleviates small intestinal inflammation. Glepaglutide can be used in the research of inflammatory bowel disease (IBD) and Crohn’s disease.

Bamadutide (SAR425899) is a potent dual glucagon-like peptide-1 receptor/glucagon receptor (GLP-1R/GCGR) agonist. Bamadutide improves post-meal blood glucose control by significantly enhancing β-cell function and slowing down the rate of glucose absorption in the body. Bamadutide can be used for the research of metabolic diseases such as type 2 diabetes.

NN1177 is a long-acting GLP-1/glucagon receptor co-agonist. NN1177 can induce a dose-dependent body weight loss in diet-induced obese (DIO) mice.

Mazdutide (IBI-362; LY-3305677) TFA is a long-acting synthetic oxyntomodulin analog. Mazdutide is also a co-agonist of glucagon-like peptide (GLP-1R) and glucagon receptor (GCGR). Mazdutide TFA 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 TFA is used in studies of obesity and type 2 diabetes (T2D).

GLP-1 receptor agonist 2 is a glucagon-like peptide-1 receptor (GLP-1R) agonist.

Enicepatide (CT-388) is a cAMP signal-biased dual GLP-1R and GIPR agonist peptide, with an EC₅₀ value of 0.087 nM for GLP-1R cAMP, and an EC₅₀ value of 2.47 nM for GIPR cAMP. Enicepatide activates the cAMP signaling pathway, while recruiting only minimal amounts of β-arrestin-2 at both targets and reducing receptor internalization levels. Enicepatide improves glycemic control, reduces body weight, suppresses appetite, and ameliorates the pathological conditions of metabolic dysfunction-associated steatohepatitis. Enicepatide can be used in the research of obesity, type 2 diabetes, and metabolic dysfunction-associated steatohepatitis.

Pegsebrenatide (NLY01) is a blood-brain barrier-penetrant GLP-1R agonist. Pegsebrenatide alleviates retinal inflammation and neuronal death secondary to ocular hypertension. Pegsebrenatide significantly delays onset and reduces disease severity in experimental autoimmune encephalomyelitis. Pegsebrenatide inhibits the formation of A1 reactive astrocytes in nerve cells and reduces the loss of retinal ganglion cells and dopaminergic neurons. Pegsebrenatide exerts neuroprotective effects in a mouse model of Parkinson's disease by directly preventing microglia-mediated conversion of astrocytes to the A1 neurotoxic phenotype. Pegsebrenatide can be used for research on glaucoma, Parkinson's disease, and multiple sclerosis.

Glucagon (22-29) is partial agonist of Glucagon (19–29). Glucagon specifically inhibits the Ca²⁺ pump in liver plasma membranes independently of adenylate cyclase activation.

SAR441255 is a GLP-1R/GCGR/GIPR agonist, with human EC₅₀ values of 1.03 pM, 1.01 pM, and 0.73 pM, respectively. SAR441255 stimulates receptor activity and drives cAMP accumulation. SAR441255 can be used for the research of type 2 diabetes, obesity.