2. Signaling Pathways
  3. GPCR/G Protein
  4. GLP Receptor

GLP Receptor

GLP Receptor

The GLP receptors contain two family members, GLP-1 receptor (GLP1R, or GLP-1R) and GLP-2 receptor (GLP2R or GLP-1R), activated by the glucagon-like peptides (GLPs). GLPs are s secreted by intestinal cells; causes insulin release; inhibits glucagon secretion, appetite, and energy intake; and delays gastric emptying because GLP receptors are located on the gut, pancreas, brainstem, hypothalamus, and vagal-afferent nerves. GLP-1 has only one known receptor, GLP1R, and regulates gut motility, appetite, islet function, and glucose homeostasis, whereas GLP-2, the agonist of GLP2R, enhances intestinal nutrient absorption. GLP-1R agonists are used to treat diabetes and obesity, and a GLP-2R agonist is approved to treat short bowel syndrome. An investigation of the actions of GLP receptor activation on gallbladder motility has demonstrated that GLP-2 receptor activation increases gallbladder volume in vivo and decreases spontaneous activity in GBSM bundles ex vivo. Like the inhibitory transmitters, which elicit their actions via an adenylate cyclase-protein kinase A-KATP channel pathway, the GLP-2 receptor signals through this same pathway.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-147629
    GLP-1R agonist 16
    		Agonist
    GLP-1R agonist 16 (Compound 115a) is a GLP-1 receptor agonist with an EC50 of 0.15 nM.
    GLP-1R agonist 16
  • HY-147627
    GLP-1R agonist 14
    		Agonist
    GLP-1R agonist 14 (Compound 14) is a GLP-1 receptor agonist with an EC50 of 0-20 nM against h-GLP-1.
    GLP-1R agonist 14
  • HY-170831
    DS79932728
    		Antagonist
    DS79932728 is an orally active inhibitor for G9a and GLP with IC50 of 12.6 nM and 75.7 nM. DS79932728 induces the production of γ-globin, thereby increasing the level of fetal hemoglobin (HbF). DS79932728 increases F-reticulocytes (F-rets) proportion and exhibits good oral absorption characteristics in cynomolgus monkey models.
    DS79932728
  • HY-162433
    I-070
    		Agonist
    I-070 is an agonist for glucagon-like peptide-1 receptor (GLP-1 receptor), with EC50 of 0.0187 nM.
    I-070
  • HY-P3506B
    Retatrutide acetate
    		Agonist
    Retatrutide (LY3437943) acetate is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide acetate inhibits human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide acetate can be used for the research of obesity.
    Retatrutide acetate
  • HY-162437
    GLP-1R agonist 22
    		Agonist
    GLP-1R agonist 22 (Compound I-135) is an agonist for glucagon-like peptide-1 receptor (GLP-1 receptor), with EC50 of 0.0165 nM.
    GLP-1R agonist 22
  • HY-114628
    MS012
    		Inhibitor
    MS012 is a selective GLP inhibitor (IC50=7 nM). MS012 can be used in research of GLP dysregulation, including cancer, inflammatory diseases, and neuroregenerative disorders.
    MS012
  • HY-P10952
    Astepatide
    		Agonist
    Astepatide is a gastric inhibitory peptide (GIP) receptor and glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in anti-diabetic research.
    Astepatide
  • HY-176493
    GLP-1R agonist 33
    		Agonist
    GLP-1R agonist 33 (Compound 224) is a GLP-1 receptor agonist. GLP-1R agonist 33 has the potential to study diabetes, obesity and non-alcoholic fatty liver disease (NAFLD).
    GLP-1R agonist 33
  • HY-176494
    WB4-24
    		Agonist
    WB4-24 is a GLP-1 receptor agonist. WB4-24 increases the release of β-endorphin in microglia. WB4-24 has anti-allergic, anti-inflammatory and analgesic effects in formalin-, carrageenan- and CFA-induced mouse inflammation models.
    WB4-24
  • HY-P11233
    Acmopatide
    		Agonist
    Acmopatide (Compound E-153) is a dual-acting GIP/GLP-1 receptor agonist. Acmopatide is used in anti-diabetic research.
    Acmopatide
  • HY-176770
    GLP-1R agonist 34
    		Agonist
    GLP-1R agonist 34 (Compound 1) is an orally active small molecule glucagon-like peptide-1 receptor (GLP-1R) agonist. GLP-1R agonist 34 promotes insulin secretion, inhibits glucagon release, and delays gastric emptying, thereby effectively lowering blood glucose levels. GLP-1R agonist 34 is promising for research of metabolic diseases, including type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).
    GLP-1R agonist 34
  • HY-155020
    Antitumor agent-101
    		Inhibitor
    Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model.
    Antitumor agent-101
  • HY-P3375A
    Mazdutide TFA
    		Agonist
    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 (Ki: 17.7 nM and 15.9 nM, respectively) and GLP-1R (Ki: 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).
    Mazdutide TFA
  • HY-P4386
    (Asp28)-Exenatide
    		Agonist
    (Asp28)-Exenatide is a degradation product of exenatide (HY-13443). (Asp28)-Exenatide can be used as a GLP-1R agonist.
    (Asp28)-Exenatide
  • HY-P10910
    Vensemaglutide
    		Agonist
    Vensemaglutide is the agonist for glucagon-like peptide 1 (GLP-1) receptor. Vensemaglutide can be used in research of diabetes or other metabolic disorders.
    Vensemaglutide
  • HY-P0165B
    Taspoglutide acetate
    		Agonist
    Taspoglutide (R1583) acetate is an agonist of the glucagon-like peptide 1 receptor (GLP-1R) with an Ki value of 1.1 nM. Taspoglutide acetate induces cAMP accumulation in CHO-K1 cells expressing human GLP-1R (EC50 = 0.06 nM). Taspoglutide acetate decreases blood levels of glucose and increases blood levels of insulin in a glucose tolerance test in Zucker diabetic obese rats. Taspoglutide acetate reduces blood levels of gastric inhibitory polypeptide (GIP), plasma levels of triglycerides, and body weight in the same model.
    Taspoglutide acetate
  • HY-172410
    GLP-1R agonist 28
    		Agonist
    GLP-1R agonist 28 (Compound 19) is an orally active GLP-1R agonist. GLP-1R agonist 28 can increase insulin secretion and can be used in the research of GLP-1R-related diseases.
    GLP-1R agonist 28
  • HY-P10965
    Zovaglutide
    		Agonist
    Zovaglutide is a GLP-1 receptor agonist and can be used for the study of diabetes.
    Zovaglutide
  • HY-P1543
    Exendin-3
    		Antagonist 98.31%
    Exendin-3 is a biologically active peptides isolated from venoms of the Gila monster lizards, Heloderma horridurn.
    Exendin-3
Cat. No. Product Name / Synonyms Application Reactivity