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-114118C
    Semaglutide sodium
    		Agonist
    Semaglutide sodium is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide sodium promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide sodium also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide sodium has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide sodium can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.
    Semaglutide sodium
  • HY-P10312
    SPN009
    		Agonist
    SPN009 (Sequence 3) is a GLP-1 Receptor agonist, with EC50 of 2.84 nM. SPN009 attenuates the type II diabetes in DB/DB mice models.
    SPN009
  • HY-13749E
    Sitagliptin hydrochloride
    		Inhibitor
    Sitagliptin (MK-0431) hydrochloride is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin hydrochloride blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin hydrochloride can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin hydrochloride shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin hydrochloride can be used for the study of 1-type and 2-type diabetes.
    Sitagliptin hydrochloride
  • HY-P10337
    OXM-7
    		Agonist
    OXM-7 is a dual agonist of GLP-1R (EC50=0.024 nM) and GCGR (EC50=0.082 nM). OXM-7 can enhance glucose-stimulated insulin secretion and hepatic glucose output. OXM-7 lowers blood glucose levels. OXM-7 improves lipid metabolism.
    OXM-7
  • HY-183693
    GLP-1 receptor agonist 21
    		Agonist
    GLP-1 receptor agonist 21 is an orally active glucagon-like peptide-1 receptor (GLP-1R) agonist with an EC50 of 0.64 nM. GLP-1 receptor agonist 21 reduces blood glucose levels and suppresses cumulative food consumption in diabetic mice. GLP-1 receptor agonist 21 can be used for the researches of type 2 diabetes and obesity.
    GLP-1 receptor agonist 21
  • HY-P3388
    Utreglutide
    		Agonist 98.42%
    Utreglutide is an effective glucagon-like peptide 1 (GLP-1) receptor agonist. Utreglutide can lower blood pressure, blood lipids and body weight, and improve cardiovascular metabolism. Utreglutide can be used for research on type 2 diabetes or non-type 2 diabetes obesity.
    Utreglutide
  • HY-145156
    CHU-128
    		Agonist
    CHU-128 is an effective and selective GLP-1R agonist. CHU-128 exhibits strong signal specificity and can activate the Gs/cAMP pathway, but it cannot activate the Gq/calcium signal, ERK phosphorylation, or recruit β-inhibitory proteins. CHU-128 can be used for research on type 2 diabetes.
    CHU-128
  • HY-W823500
    GLP-1R agonist 39
    		98.37%
    GLP-1R agonist 39 (Compound 7) is a potent GLP-1 receptor positive allosteric modulator. GLP-1R agonist 39 can be used for the research of obesity and type 2 diabetes.
    GLP-1R agonist 39
  • HY-181709
    TPM003
    		Agonist
    TPM003 (TG062) is a triple agonist of GLP-1R, GIPR and GCGR, with EC50 values of 33.9, 12.5 and 92.9 pM, respectively. TPM003 suppresses appetite, regulates blood glucose, enhances insulin sensitivity, reduces gastrointestinal intolerance, promotes hepatic lipid mobilization and increases energy expenditure. TPM003 induces weight loss, improves metabolic parameters, reverses hepatic steatosis and optimizes liver function markers. TPM003 is applicable for research on obesity and non-alcoholic steatohepatitis.
    TPM003
  • HY-13749R
    Sitagliptin (Standard)
    		Inhibitor
    Sitagliptin (Standard) is the analytical standard of Sitagliptin (HY-13749). This product is intended for research and analytical applications. Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
    Sitagliptin (Standard)
  • HY-180489
    GLP-1R agonist 38
    		Agonist
    GLP-1R agonist 38 (page 15, compound 1) is a glucagon-like peptide-1 receptor (GLP-1R) agonist. GLP-1R agonist 38 can be used for the study of metabolic disorders and related diseases, including but not limited to type II diabetes mellitus (T2DM), obesity and non-alcoholic fatty liver disease (NASH).
    GLP-1R agonist 38
  • HY-P0119S
    Lixisenatide (Leu-13C6,15N) TFA
    		Agonist
    Lixisenatide (Leu-13C6,15N) TFA is the 13C- and 15N-labeled Lixisenatide (HY-P0119). Lixisenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of pro-inflammatory cytokines, and suppresses of the Akt-MEK1/2 signaling pathway. Lixisenatide can inhibit oxidative stress, mitochondrial dysfunction and apoptosis. Lixisenatide 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.
    Lixisenatide (Leu-<sup>13</sup>C<sub>6</sub>,<sup>15</sup>N) TFA
  • HY-13749S3
    Sitagliptin-d6
    		Inhibitor
    Sitagliptin-d6 (MK-0431-d6) is deuterium labeled Sitagliptin (HY-13749). Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
    Sitagliptin-d<sub>6</sub>
  • HY-181257
    GLP-1 receptor agonist 18
    		Agonist
    GLP-1 receptor agonist 18 is an orally active GLP-1 receptor agonist with an EC50 of 0.22 nM. GLP-1 receptor agonist 18 can reduces blood sugar levels and body weight. GLP-1 receptor agonist 18 can be used for the research of diabetes.
    GLP-1 receptor agonist 18
  • HY-P0014AS
    Liraglutide-d8 tetraTFA
    		Agonist
    Liraglutide-d8 tetraTFA is deuterium labeled Liraglutide (HY-P0014). Liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist used for the study of type 2 diabetes mellitus.
    Liraglutide-d<sub>8</sub> tetraTFA
  • HY-180220
    GLP-1R agonist 40
    		Agonist
    GLP-1R agonist 40 (Compound I-1) is an orally active, potent and selective GLP-1R agonist (EC50 = 26.7 pM for cAMP accumulation). GLP-1R agonist 40 shows significant decrease in blood glucose levels. GLP-1R agonist 40 can be used in the research of type 2 diabetes.
    GLP-1R agonist 40
  • HY-168585
    GLP-1R agonist 26
    		Agonist
    GLP-1R agonist 26 (compound 1) is a glucagon-like peptide-1 receptor (GLP-1R) agonist with an EC50 of <10 nM.
    GLP-1R agonist 26
  • HY-172411
    GLP-1R agonist 29
    		Agonist
    GLP-1R agonist 29 (Compound 20) is the agonist for GLP-1R that induces hGLP-1R mediated cAMP stimulation with an EC50 of 0.018 nM. GLP-1R agonist 29 exhibits good pharmacokinetics characteristics with good body exposure of AUC0-∞,sc of 77688 ng·h/mL.
    GLP-1R agonist 29
  • HY-108795R
    Albiglutide fragment (Standard)
    		Agonist
    Albiglutide fragment (Standard) is the analytical standard of Albiglutide fragment (HY-108795). This product is intended for research and analytical applications. 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 (Standard)
  • HY-13749BR
    Sitagliptin phosphate monohydrate (Standard)
    		Inhibitor
    Sitagliptin (MK-0431) phosphate monohydrate (Standard) is the analytical standard of Sitagliptin phosphate monohydrate (HY-13749B). This product is intended for research and analytical applications. Sitagliptin phosphate monohydrate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate monohydrate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate monohydrate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate monohydrate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate monohydrate can be used for the study of 1-type and 2-type diabetes.
    Sitagliptin phosphate monohydrate (Standard)
Cat. No. Product Name / Synonyms Application Reactivity