GLP Receptor Agonist

Semaglutide, Cy5-labeled (Semaglutide-Cys(Cy5)) is a CY5 (HY-D0821) -labeled version of Semaglutide (HY-114118) (Ex/Em = 633/670 nm). Semaglutide, Cy5-labeled can be used for studies on Semaglutide receptor binding (GLP-1R), cellular uptake and endocytosis, in vivo tissue distribution, and the targeting efficiency of delivery systems.

Berobenatide (PF-08653944; MET-097) is a GLP-1R agonist that exerts functional regulation of GLP-1R biased toward the Gs protein signaling pathway. Berobenatide induces weight loss in diet-induced obese mice. Berobenatide can be used in obesity-related research.

GCGR/GLP‐1 receptor agonist P1 is a dual GCGR/GLP-1R agonist. GCGR/GLP‐1 receptor agonist P1 activates human GCGR in vitro and induces the cyclic adenosine monophosphate (cAMP) signaling pathway. GCGR/GLP‐1 receptor agonist P1 is applicable to research related to type 2 diabetes and obesity.

GLP-1R agonist 23 (Example 376) is a GLP-1R agonist with an EC₅₀ of 0.056 nM. GLP-1R agonist 23 can be used in diabetes research.

GLP-1R agonist 13 (Compound 24) is a GLP-1 receptor agonist.

Caroglipron (GLP-1 receptor agonist 16) (Example 53) is a GLP-1 agonist. Caroglipron can be used for the research of diabetes, obesity, or nonalcoholic steatohepatitis-related diseases^[1].

GLP-1R agonist 30 is a selective and orally active GLP-1R agonist with an EC₅₀ of 0.048 nM. GLP-1R has excellent selectivity, with EC₅₀ greater than 20 μM for GLP-2R, GIPR, and GCPR. GLP-1R agonist significantly increases cAMP-stimulating activity while markedly reducing hERG inhibitory activities. GLP-1R agonist has preferable absorption and excellent β-arrestin pathway selectivity. GLP-1R agonist effectively improves glucose tolerance and promoted insulin secretion in B-hGLP1R knock-in mice.

Semaglutide sodium is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide sodium promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide sodium also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide sodium has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide sodium can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.

SPN009 (Sequence 3) is a GLP-1 Receptor agonist, with EC₅₀ of 2.84 nM. SPN009 attenuates the type II diabetes in DB/DB mice models.

IUB0271 (acyl-GIP) is a glucose-dependent insulinotropic polypeptide receptor (GIPR) agonist with blood-brain barrier permeability. IUB0271 activates the GIPR signaling pathway, inhibits food intake and weight gain, and induces cFos neuron activation in the area postrema. IUB0271 enhances lipid clearance and induces systemic fatty acid oxidation. IUB0271 improves dyslipidemia, reduces atherosclerotic plaque formation and decreases adipocyte volume. IUB0271 can be used in studies related to obesity, dyslipidemia and atherosclerosis.

OXM-7 is a dual agonist of GLP-1R (EC₅₀=0.024 nM) and GCGR (EC₅₀=0.082 nM). OXM-7 can enhance glucose-stimulated insulin secretion and hepatic glucose output. OXM-7 lowers blood glucose levels. OXM-7 improves lipid metabolism.

GLP-1 receptor agonist 21 is an orally active glucagon-like peptide-1 receptor (GLP-1R) agonist with an EC₅₀ of 0.64 nM. GLP-1 receptor agonist 21 reduces blood glucose levels and suppresses cumulative food consumption in diabetic mice. GLP-1 receptor agonist 21 can be used for the researches of type 2 diabetes and obesity.

Utreglutide is an effective glucagon-like peptide 1 (GLP-1) receptor agonist. Utreglutide can lower blood pressure, blood lipids and body weight, and improve cardiovascular metabolism. Utreglutide can be used for research on type 2 diabetes or non-type 2 diabetes obesity.

CHU-128 is an effective and selective GLP-1R agonist. CHU-128 exhibits strong signal specificity and can activate the Gs/cAMP pathway, but it cannot activate the Gq/calcium signal, ERK phosphorylation, or recruit β-inhibitory proteins. CHU-128 can be used for research on type 2 diabetes.

GLP-1 receptor agonist 24 is a glucagon-like peptide-1 receptor (GLP-1R) agonist. GLP-1 receptor agonist 24 activates the GLP-1R signaling pathway and regulates glucose metabolism-related responses, including glucose-stimulated insulin secretion and metabolic homeostasis. GLP-1 receptor agonist 24 can be used in studies of metabolism-related diseases.

Tapimtrutide is a gastric inhibitory polypeptide (GIP) and glucagon-like peptide 1 (GLP-1) receptor agonist. Tapimtrutide can be used for the research of diabetes.

Zormapatide is a gastric inhibitory polypeptide (GIP) receptor agonist peptide. Zormapatide contains 2-methylalanine residues and an N⁶-[N-(19-carboxynonadecanoyl)-L-γ-glutamyl-L-lysyl] modification. Zormapatide is applicable to the research of diabetes and metabolic diseases.

TPM003 (TG062) is a triple agonist of GLP-1R, GIPR and GCGR, with EC₅₀ values of 33.9, 12.5 and 92.9 pM, respectively. TPM003 suppresses appetite, regulates blood glucose, enhances insulin sensitivity, reduces gastrointestinal intolerance, promotes hepatic lipid mobilization and increases energy expenditure. TPM003 induces weight loss, improves metabolic parameters, reverses hepatic steatosis and optimizes liver function markers. TPM003 is applicable for research on obesity and non-alcoholic steatohepatitis.

Retatrutide, Pro40(¹³C₅,¹⁵N) (LY3437943, Pro40(¹³C₅,¹⁵N) 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 38 (page 15, compound 1) is a glucagon-like peptide-1 receptor (GLP-1R) agonist. GLP-1R agonist 38 can be used for the study of metabolic disorders and related diseases, including but not limited to type II diabetes mellitus (T2DM), obesity and non-alcoholic fatty liver disease (NASH).