GLP Receptor Agonist

Naperiglipron (LY3549492) is an orally active Glucagon-like peptide 1 receptor (GLP-1R) agonist with an EC₅₀ of 1.14 nM for hGLP-1R. Naperiglipron significantly decreases the level of blood glucose in GLP-1R knock-in mouse models. Naperiglipron inhibits PDE10A1 enzyme activity (IC₅₀: 7.43 μM) with a weak hERG inhibitory activity. Naperiglipron can be used for type II diabetes mellitus (T2DM) and obesity research.

(4S)-GLP-1 receptor agonist 14 is a potent and orally active GLP-1 receptor agonist with an EC₅₀ ≤ 20 nM. (4S)-GLP-1 receptor agonist 14 can be used for research on diabetes, obesity, metabolic diseases, cardiovascular diseases, liver diseases, nonalcoholic steatohepatitis (NASH), and other diseases associated with GLP-1 receptor.

Albiglutide fragment (GLP-1 (7-36) analog) is an active fragment of Albiglutide (7-36) and a glucagon-like peptide-1 (GLP-1) analog (a long-acting GLP-1 receptor agonist). Albiglutide is produced by the fusion of DPP-4 resistant GLP-1 dimer with the human albumin gene. Moreover, Albiglutide fragment significantly reduces glycosylated hemoglobin (A1C) and is used in type 2 diabetes (T2D) studies.

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.

Brenipatide (LY-3537031) is a dual glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP) receptor agonist. Brenipatide can be used for the study of metabolic disorders, obesity and diabetes.

GLP-1 receptor agonist 11 is a GLP-1 receptor agonist.GLP-1 receptor agonist 11 activates the GLP-1 receptor.GLP-1 receptor agonist 11 can be used for the research of diabetes, non-alcoholic fatty liver disease, glucose intolerance, dyslipidemia, syndrome x, arteriosclerosis, hypertension, obesity, hepatic fibrosis, cirrhosis, somnolence, hyperglycemia, hyperlipidemia, atherosclerosis, hypertriglyceridemia, type 1 diabetes, type 2 diabetes, diabetic dyslipidemia.

Liraglutide (TFA) is an agonist of glucagon-like peptide 1 receptor (GLP-1). Liraglutide (TFA) can activate GLP-1, leading to the release of insulin in the presence of increased glucose concentration. Liraglutide (TFA) also reduces glucagon secretion in a glucose-dependent manner. Liraglutide (TFA) can be studied in research on type 2 diabetes.

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.

DD202-114 is a potent and selective GLP1R agonist. DD202-114 inhibits hERG with an IC₅₀ of 15.9 μM. DD202-114 exhibits strong CYP2C8 inhibition with an IC₅₀ of 0.22 μM. DD202-114 promotes cAMP accumulation. DD202-114 reduces blood glucose levels and food intake. DD202-114 has the potential to be used in the study of type 2 diabetes mellitus (T2DM) and obesity.

Lixisenatide acetate is a glucagon-like peptide-1 (GLP-1) receptor agonist. Lixisenatide acetate inhibits the inflammatory response through down regulation of pro-inflammatory cytokines, and suppresses of the Akt-MEK1/2 signaling pathway. Lixisenatide acetate can inhibit oxidative stress, mitochondrial dysfunction and apoptosis. Lixisenatide acetate can be used for the researches of inflammation, metabolic disease, neurological disease and cardiovascular disease, such as rheumatoid arthritis, diabetes, Alzheimer's disease and atherosclerosis.

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 7 is a heterocyclic glucagon-like peptide-1 receptor (GLP-1 receptor) agonist, which can be used in glucose metabolism-related research.

GLP-1R agonist 10 is a heterocyclic GLP-1R agonist. GLP-1R agonist 10 can be used for the research of type 2 diabetes mellitus.

PF-06954522 is a glucagon-like peptide-1 receptor (GLP-1R) agonist. PF-06954522 is applicable to research related to type 2 diabetes.

Semaglutide-FITC (Semaglutide-Lys(FITC)) is a fluorescent tracer probe (Ex/Em = 495/520 nm) obtained by covalently coupling the green fluorescent dye fluorescein isothiocyanate (FITC) (HY-66019) to the long-acting analogue of GLP-1, Semaglutide (HY-114118). Semaglutide-FITC can be used for studies on Semaglutide receptor binding (GLP-1R), cell uptake and endocytosis, in vivo tissue distribution, and the targeting efficiency of delivery systems.

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

Bofanglutide (GZR18) is an analog of glucagon-like peptide-1 (GLP-1), which exhibits agonistic activity for GLP-1 receptor, with an EC₅₀ of 0.677 nM. GZR18 ameliorates type 2 diabetes.

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.