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.

GLP Receptor Related Products (201)
Antibodies (1)

By Effects:	Inhibitors (16) Agonists (126) Degraders (2) Controls (2) Ligand (1) Antagonists (8) Activators (13) Modulators (8) Inducer (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-P11881

IUB288	Agonist
IUB288 is a stable and long-acting glucagon-modified peptide, as well as a highly selective Glucagon Receptor agonist. IUB288 stimulates the production of cAMP, increases the expression levels of FGF21 in plasma and liver, regulates bile acid metabolism, and inhibits the expression of hepatic HMGCR. IUB288 improves hypercholesterolemia, enhances insulin sensitivity, increases core body temperature, boosts energy expenditure, suppresses food intake, and can also induce hyperglycemia and glucose intolerance. IUB288 is applicable to the research of diet-induced obesity, type 2 diabetes, and obesity-related glucose intolerance.

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).

HY-153476

GIP/GLP-1 dual receptor agonist-1	Agonist
GIP/GLP-1 dual receptor agonist-1 is a GIP/GLP-1 dual receptor agonist. GIP/GLP-1 dual receptor agonist-1 is used in the research of metabolic disorders and fatty liver diseases, including non-alcoholic steatohepatitis (NASH) and non-alcoholic fatty liver disease (NAFLD).

HY-P11262

GUB021794	Agonist
GUB021794 is a potent and highly selective glucagon-like peptide-1 receptor (GLP-1R) agonist developed using the streaMLine platform with an EC₅₀ value of 18 pM. GUB021794 has a very weak activity against SCTR, with an EC₅₀ value of 190 nM. GUB021794 can significantly reduce the body weight, food intake, and total fat mass of mice in a diet-induced obesity (DIO) model. GUB021794 can be used for research on obesity/diabetes.

HY-P11233

Acmopatide	Agonist
Acmopatide (Compound E-153) is a dual-acting GIP/GLP-1 receptor agonist. Acmopatide is used in anti-diabetic research.

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).

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.

HY-178768

GLP-1R agonist 35	Antagonist
GLP-1R agonist 35 (Compound 111-2) is a GLP-1R agonist with an EC₅₀ of 0-10 nM. GLP-1R agonist 36 can be used for the studies of diabetes and obesity.

HY-101122

LX2761	Activator
LX2761 is an orally active, dual SGLT1/SGLT2 inhibitor with IC₅₀ values of 2.2 nM and 2.7 nM against human SGLT1 and SGLT2, respectively. LX2761 locks human SGLT1 in an outward-open conformation and blocks its putative water permeation pathway. After oral administration, LX2761 is confined exclusively to the intestinal lumen, delays intestinal glucose absorption, regulates intestinal glucose metabolism, increases cecal glucose levels, reduces cecal pH, improves glycemic control and elevates plasma total GLP-1 levels. However, LX2761 induces diarrhea in a dose-dependent manner. LX2761 can be used in diabetes-related research.

HY-171302

GLP-1R/GIPR agonist-2	Agonist
GLP-1R/GIPR agonist-2 is a GIPR agonist. GLP-1R/GIPR agonist-2 potentiates GIP(1-42)-induced intracellular cAMP production in cells expressing human GIPR. GLP-1R/GIPR agonist-2 can be used for the research of type II diabetes mellitus.

HY-10289

Carmegliptin	Activator
Carmegliptin (RO-4876904) is an orally active and potent DPP IV inhibitor with a human DPP IV IC₅₀ of 6.8 nM. Carmegliptin 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 acts as a substrate for human P glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin can be used for the research of type 2 diabetes, non insulin dependent diabetes mellitus.

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.

HY-182849

GLP-1R agonist 44	Agonist
GLP-1R agonist 44 is a glucagon-like peptide-1 receptor (GLP-1R) agonist. GLP-1R agonist 44 can be used for the research of diseases related to GLP-1R, such as type 2 diabetes, obesity, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, nephropathy, gout, hematuria, cardiovascular disease.

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.

HY-P0165B

Taspoglutide acetate	Agonist
Taspoglutide (R1583) acetate is an agonist of the glucagon-like peptide 1 receptor (GLP-1R) with an K_i 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.

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.

HY-115643

AZ13581837	Inducer
AZ13581837 is an orally active GPR120 agonist with an EC₅₀ of 5.2 nM for human GPR120. AZ13581837 signals through Gαq, Gαs, and β-arrestin pathways, reduces cAMP production, stimulates GLP-1 secretion, induces glucose lowering, and increases insulin secretion. AZ13581837 can be used for the research of type 2 diabetes.

HY-182300

FE 999011	Activator
FE 999011 is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor with IC₅₀ values of 7 nM and 3 nM against human and rat sources, respectively. FE 999011 acts as a glucose tolerance-improving agent and a GLP-1 receptor activator, which reduces blood glucose fluctuation, promotes GLP-1 release and decreases the insulin-glucose ratio. FE 999011 regulates lipid metabolism, delays the onset of diabetes, stabilizes food and water intake, reduces hypertriglyceridemia, prevents the elevation of free fatty acids, and delays the progression of impaired glucose tolerance to disease. FE 999011 can be used in relevant studies of type 2 diabetes.

HY-N18033

Glyceollin III
Glyceollin III is a glyceollin found in soybeans. Glyceollin III enhances insulin-stimulated glucose uptake and increases glucagon-like peptide-1 (GLP-1) secretion. Glyceollin III can be used for the research of type 2 diabetes.

HY-P11664

Anvoglutide	Agonist
Anvoglutide is a glucagon-like peptide 1 (GLP-1) receptor agonist with antidiabetic and obesity effects.

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GLP Receptor

GLP Receptor Related Products (201)

Antibodies (1)

GLP Receptor Related Products (201):