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-P10327
    PP18
    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-162362
    MS8709
    		Degrader
    MS8709 (10), a potential anticancer therapeutic, is a first-in-class G9a/GLP PROTAC degrader. MS8709 (10) is based on G9a/GLP inhibitor UNC0642 and recruits the von Hippel Lindau (VHL) E3 ligase (Red: G9a/GLP inhibitor UNC0642; Blue: VHL ligand; Black: linker).
    MS8709
  • 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
  • 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-P10031
    SAR441255
    		Agonist
    SAR441255 is a potent unimolecular peptide GLP-1/GIP/GCG receptor triagonist. SAR441255 displays high potency with balanced activation of all three target receptors.?SAR441255 shows positive acute glucoregulatory effectss in diabetic obese monkeys.
    SAR441255
  • HY-153193
    LSN3160440
    		Modulator
    LSN3160440 is an allosteric modulator of GLP-1R, which acts as a protein–protein interaction (PPI) stabilizer or molecular glue to assist in the adhesion of inactive GLP-1 (9-36) NH2 on GLP-1R.
    LSN3160440
  • HY-162434
    I-128
    		Agonist
    I-128 is an agonist for glucagon-like peptide-1 receptor (GLP-1 receptor), with EC50 of 0.0122 nM.
    I-128
  • HY-147626
    GLP-1R agonist 13
    		Agonist
    GLP-1R agonist 13 (Compound 24) is a GLP-1 receptor agonist.
    GLP-1R agonist 13
Cat. No. Product Name / Synonyms Application Reactivity