1. Signaling Pathways
  2. GPCR/G Protein
  3. 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-162436
    GLP-1R agonist 21
    Agonist
    GLP-1R agonist 21 (Compound I-134) is an agonist for glucagon-like peptide-1 receptor (GLP-1 receptor), with EC50 of 0.0104 nM.
    GLP-1R agonist 21
  • HY-160734
    Aleniglipron
    Agonist
    Aleniglipron (compound 121a) is a GLP-1 agonist with an EC50 value of less than 0.1 nM in the HDB cell line in a cAMP stimulation assay.
    Aleniglipron
  • HY-160031
    GLP-1R agonist 19
    Agonist
    GLP-1R agonist 19 (M3190) is a potent and selective GLP-1R agonist. GLP-1R agonist 19 has excellent plasma stability, liver microsomal stability, and low hERG toxicity.
    GLP-1R agonist 19
  • HY-162435
    GLP-1R agonist 20
    Agonist
    GLP-1R agonist 20 (Compound I-132) is an agonist for glucagon-like peptide-1 receptor (GLP-1 receptor), with EC50 of 0.0162 nM.
    GLP-1R agonist 20
  • HY-P10327
    PP18
    Agonist
    PP18 is a novel OXM-based dual GLP-1 and glucagon receptor agonist with EC50 values of 0.487 nM target hGLP-1R and 0.188 nM target hGcgR.
    PP18
  • HY-108795
    Albiglutide fragment
    Agonist
    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.
    Albiglutide fragment
  • HY-143312B
    (R)-V-0219
    Modulator
    (R)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 activates calcium fluxes in HEK cells stably expressing hGLP-1R.
    (R)-V-0219
  • HY-P10592
    Bofanglutidum
    Agonist
    Bofanglutide (Bofanglutidum) is a glucagon-like peptide 1 (GLP-1) receptor agonist.
    Bofanglutidum
  • HY-120828
    Albenatide
    Agonist
    Albenatide (CJC 1134PC) is a modified Exendin-4 (HY-13443) analogue conjugated to human recombinant albumin (HRA) in vitro to form a long-acting DPP-4-resistant GLP-1R agonist. Albenatide covalently binds through a low-molecular chemical linker (cys-C13H19O6N3-lys) to the cysteine residue in position 34 of HRA. Albenatide increases cyclic AMP (cAMP) production in vitro. Albenatide reduces glucose excursions, food intake, gastric emptying in wild-type mice and improves glucose tolerance and reduces body weight in high-fat diet mice.
    Albenatide
  • 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-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-P10032
    NN1177
    Agonist
    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.
    NN1177
  • 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-P5815
    GLP-1 (1-36) amide (human, rat)
    GLP-1 (1-36) amide (human, rat) (Glucagon-like Peptide 1 (1-36) amide (human, rat) ) is a molecular variant of glucagon-like peptide 1 (GLP-1)-(7-36) amide. GLP-1 (1-36) amide (human, rat) can stimulate [14C]aminopyrine accumulation on enzymatically dispersed enriched rat parietal cells.
    GLP-1 (1-36) amide (human, rat)
  • HY-P10269
    GZR18
    Agonist
    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.
    GZR18
  • 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
Cat. No. Product Name / Synonyms Application Reactivity