GCGR 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.

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.

GLP-1R agonist 7 is a potent GLP-1R agonist with an EC₅₀ of 0.67 µM (WO2021244645A1, compound WXA001).

FC382K10W15 TFA is a glucagon analogue and GLP-1R/GCGR agonist. FC382K10W15 TFA can be used in type 2 diabetes research.

Retatrutide, Phe22(¹³C₉,¹⁵N) (LY3437943, Phe22(¹³C₉,¹⁵N) TFA is the ¹³C, ¹⁵N-labeled Retatrutide (HY-P3506). 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.

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).

Retatrutide (LY3437943) (crude) is the crude form of Retatrutide (HY-P3506). Retatrutide 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.

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-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.

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.

Neuropeptide Y, porcine, a peptide in porcine brain, is capable of inhibiting secretin-stimulated pancreatic secretion.

GLP-1R agonist 8 is a potent GLP-1R agonist with an EC₅₀ of < 2 nM (WO2021219019A1, compound 129a).

IUB288 is a stable and long-acting glucagon-modified peptide, as well as a highly selective Glucagon Receptor agonist. IUB288 stimulates the production of cAMP, increases the expression levels of FGF21 in plasma and liver, regulates bile acid metabolism, and inhibits the expression of hepatic HMGCR. IUB288 improves hypercholesterolemia, enhances insulin sensitivity, increases core body temperature, boosts energy expenditure, suppresses food intake, and can also induce hyperglycemia and glucose intolerance. IUB288 is applicable to the research of diet-induced obesity, type 2 diabetes, and obesity-related glucose intolerance.

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

GIP/GLP-1 dual receptor agonist-1 is a GIP/GLP-1 dual receptor agonist. GIP/GLP-1 dual receptor agonist-1 is used in the research of metabolic disorders and fatty liver diseases, including non-alcoholic steatohepatitis (NASH) and non-alcoholic fatty liver disease (NAFLD).

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).

TT-OAD2 free base is a non-peptide glucagon-like peptide-1 (GLP-1) receptor agonist with an EC₅₀ of 5 nM. TT-OAD2 free base has the potential for diabetes treatment.

GLP-1R agonist 31 (Compound 1) is an amorphous glucagon-like peptide-1 receptor (GLP-1R) agonist.

GLP-1R agonist 5 is a potent GLP-1R agonist with an EC₅₀ of <10 nM (WO2021259309A1, compound 35).

UTG-4 is a GLP-1R, GIPR, and GCGR agonist with EC₅₀ values of 126.3 pM, 29.2 pM, and 250.2 pM, respectively. UTG-4 binds to HSA (K_d = 14.6 μM). UTG-4 effectively alleviates endothelial-mesenchymal transition. UTG-4 promotes weight loss, inhibits food intake, improves glucose tolerance, and has a significant anti-atherosclerotic effect.