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-P4610
    H-Trp-Tyr-OH
    Activator 99.43%
    H-Trp-Tyr-OH is an orally active tryptophan-tyrosine dipeptide with blood-brain barrier permeability. H-Trp-Tyr-OH exerts physiological regulatory effects by stimulating enteroendocrine cells to secrete glucagon-like peptide GLP-1. In mouse models of tauopathies, H-Trp-Tyr-OH inhibits tau phosphorylation, reduces the level of neurofibrillary tangles, increases dopamine turnover, upregulates synapsin expression, and elevates cecal short-chain fatty acid levels, thereby improving behavioral deficits and extending lifespan. H-Trp-Tyr-OH can be used in research related to impaired glucose tolerance and tauopathies.
    H-Trp-Tyr-OH
  • HY-171850
    GLP-1R modulator-1
    Agonist
    GLP-1R modulator-1 (Compound 384) is an orally active, potent selective glucagon-like peptide-1 receptor (GLP-1R) agonist. GLP-1R modulator-1 activates G-protein coupled signaling, elevates intracellular cAMP levels, promotes insulin secretion, delays gastric emptying and suppresses appetite. GLP-1R modulator-1 is promising for research of type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).
    GLP-1R modulator-1
  • HY-P0014A
    Liraglutide acetate
    Agonist
    Liraglutide acetate is the acetate form of Liraglutide (HY-P0014), a glucagon-like peptide-1 (GLP-1) receptor agonist studied in type 2 diabetes.
    Liraglutide acetate
  • HY-P10842
    d-GLP-2 E33A
    Agonist
    d-GLP-2 E33A is an agonist for the glucagon-like peptide 2 receptor (GLP-2R) with an EC50 of 414 nM. d-GLP-2 E33A can activate GLP-2R and increase the phosphorylation of AKT, but has no stimulative effect on GLP-1R. d-GLP-2 E33A can be used in the study of diseases such as intestinal malabsorption and inflammatory bowel diseases.
    d-GLP-2 E33A
  • HY-P11487
    UTG-4
    Agonist
    UTG-4 is a GLP-1R, GIPR, and GCGR agonist with EC50 values of 126.3 pM, 29.2 pM, and 250.2 pM, respectively. UTG-4 binds to HSA (Kd = 14.6 μM). UTG-4 effectively alleviates endothelial-mesenchymal transition. UTG-4 promotes weight loss, inhibits food intake, improves glucose tolerance, and has a significant anti-atherosclerotic effect.
    UTG-4
  • HY-182502
    GLP-1R-agonist-43
    Agonist
    GLP-1R-agonist-43 (Compound A) is an orally active GLP-1R agonist with an EC50 of 2.68 nM. GLP-1R-agonist-43 can be used in the research of non-insulin-dependent diabetes mellitus (type 2 diabetes) and obesity.
    GLP-1R-agonist-43
  • HY-178769
    GLP-1R agonist 36
    Agonist
    GLP-1R agonist 36 (Compound 53) is a GLP-1R agonist with a total of four isomers. GLP-1R agonist 36 can be used for the studies of diabetes and obesity.
    GLP-1R agonist 36
  • HY-176838
    LXT34
    LXT34 (Example 2) is a GPR120 agonist. LXT34 has an anti-inflammatory activity. LXT34 promotes GLP-1 formation in the gastrointestinal tract and improves insulin resistance in macrophages and pancreas cells. LXT34 can be used for inflammatory diseases, such as type 2 diabetes, obesity and non-alcoholic fatty liver research.
    LXT34
  • HY-162434
    GLP-1R agonist 42
    Agonist
    GLP-1R agonist 42 is an agonist for glucagon-like peptide-1 receptor (GLP-1 receptor), with EC50 of 0.0122 nM.
    GLP-1R agonist 42
  • HY-P11279
    TC2
    Agonist
    TC2 is an efficient GIPR-preferring monomeric quadruple agonist that can respectively activate GIPR, GLP-1R, GcgR, and Y2R with IC50 values of 0.47, 2.1, 30, and 55 nM respectively. TC2 exhibits a significant GLP-1R preference, with a significant reduction in β-inhibitory protein 2 (βArr2) recruitment, while maintaining a strong cAMP signal. TC2 can be used for research on obesity and diabetes.
    TC2
  • HY-P11667
    Erzemdutide
    Agonist
    Erzemdutide is a glucagon and glucagon-like peptide 1 (GLP-1) receptor agonist. Erzemdutide can be used for the study of obesity.
    Erzemdutide
  • HY-114118F5
    Semaglutide, Cy5 labeled
    Agonist
    Semaglutide, Cy5 labeled is a CY5 (HY-D0821) labeled Semaglutide (HY-114118), which is suitable for high-sensitivity fluorescence detection and imaging (Ex/Em = 633/670 nm).
    Semaglutide, Cy5 labeled
  • HY-P11235
    Berobenatide
    Agonist
    Berobenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist.
    Berobenatide
  • HY-W701772
    2-Oleoylglycerol-d5
    2-Oleoylglycerol-d5 (2-OG-d5) is the deuterium labeled 2-Oleoylglycerol (HY-W011121). 2-Oleoylglycerol (2-OG) is a lipid found in the diet. It is a GPR119 agonist, with an EC50 value of 2.5 μM in activating hGPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol enhances the inflammatory response of macrophages and promotes fibrosis by activating the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. It also stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. 2-Oleoylglycerol is expected to be used in the research of non-alcoholic steatohepatitis (NASH) .
    2-Oleoylglycerol-d<sub>5</sub>
  • HY-161915
    GLP-1R agonist 23
    Agonist
    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 23
  • HY-147626
    GLP-1R agonist 13
    Agonist
    GLP-1R agonist 13 (Compound 24) is a GLP-1 receptor agonist.
    GLP-1R agonist 13
  • HY-10289A
    Carmegliptin hydrochloride
    Activator
    Carmegliptin hydrochloride (RO-4876904 hydrochloride) is an orally active and potent DPP‑IV inhibitor with a human DPP‑IV IC50 of 6.8 nM. Carmegliptin hydrochloride binds to the S1 pocket of DPP‑IV, blocks the degradation of GLP‑1, potentiates endogenous GLP‑1, increases plasma insulin levels, alleviates hyperglycemia, improves glucose tolerance. Carmegliptin hydrochloride acts as a substrate for human P‑glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin hydrochloride can be used for the research of type 2 diabetes, non‑insulin‑dependent diabetes mellitus.
    Carmegliptin hydrochloride
  • HY-P4389
    (Asp28)-Glucagon (1-29) (human, rat, porcine)
    Activator
    (Asp28)-Glucagon (1-29) (human, rat, porcine) is an optimized structure of glucagon, the 28th position is replaced by aspartic acid (Asp) which significantly increases the aqueous solubility of glucagon in a physiological pH buffer, has the same activity as glucagon.
    (Asp28)-Glucagon (1-29) (human, rat, porcine)
  • HY-170516
    GLP-1 receptor agonist 16
    Agonist
    GLP-1 receptor agonist 16 (Example 53) is a GLP-1 agonist. GLP-1 receptor agonist 16 can be used for the research of diabetes, obesity, or nonalcoholic steatohepatitis-related diseases[1].
    GLP-1 receptor agonist 16
  • HY-173479
    GLP-1R agonist 30
    Agonist
    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.
    GLP-1R agonist 30
Cat. No. Product Name / Synonyms Application Reactivity