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-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.

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.

HY-178378

G9a-IN-4	Inhibitor
G9a-IN-4 is a G9a inhibitor with high selectivity (IC₅₀ = 32 nM). G9a-IN-4 shows high selectivity against the other tested lysine/arginine methyltransferases. G9a-IN-4 exhibits high enzymatic activity against G9a and more potent antiproliferative effects against all tested cancer cells. G9a-IN-4 significantly suppresses the H3K9me2 level. G9a-IN-4 triggers autophagy by inducing the production of ROS, thus leading to cell apoptosis and cell cycle arrest at G0/G1 in CT26 colon cells. G9a-IN-4 can be used for the study of colon cancer.

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.

HY-168481

GLP-1R agonist 27	Agonist
GLP-1R agonist 27 (compound 21) is a potent and orally active GLP-1R agonist. GLP-1R agonist 27 promots cyclic adenosine monophosphate (cAMP) accumulation. GLP-1R agonist 27 reduces blood glucose levels and food intake. GLP-1R agonist 27 has the potential for the research of obesity and type 2 diabetes mellitus (T2DM).

HY-182336

DeDPP4	Activator
DeDPP4 is a DPP-4 PROTAC degrader. DeDPP4 induces sustained elevation of glucagon-like peptide-1 (GLP-1), enhances glucose tolerance, causes persistent reduction of blood glucose, and achieves long-term blood glucose regulation in animal models of type 2 diabetes. DeDPP4 mediates dose-dependent DPP-4 depletion in cancer cells, and also targets and degrades DPP-4 in the liver and adipose tissues of animal models with type 2 diabetes. DeDPP4 can be used for the research of type 2 diabetes and non-small cell lung cancer.

HY-P11042

TE-8105	Agonist
TE-8105 is a GLP-1 receptor agonist that has demonstrated prolonged and potent efficacy in models of diabetes, obesity, and non-alcoholic steatohepatitis (NASH).

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.

HY-175420

K-757	Modulator
K-757 is a GPR40 agonist with an EC₅₀ of 2.1 ± 0.2 nM for human GPR40. K-757 exhibits a half-life of 1-11 h in Preclinical Species. K-757 stimulates GLP-1 secretion and has potential applications in bariatric research.

HY-P11673

Zabopegdutide	Agonist
Zabopegdutide is a glucagon and glucagon-like peptide 1 (GLP-1) receptor agonist. Zabopegdutide can be used for the study of obesity.

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.

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.

HY-170831

DS79932728	Antagonist
DS79932728 is an orally active inhibitor for G9a and GLP with IC₅₀ of 12.6 nM and 75.7 nM. DS79932728 induces the production of γ-globin, thereby increasing the level of fetal hemoglobin (HbF). DS79932728 increases F-reticulocytes (F-rets) proportion and exhibits good oral absorption characteristics in cynomolgus monkey models.

HY-179332

GIPR antagonist 1
GIPR antagonist 1 is a GIPR antagonist with an IC₅₀ of 4.8 nM. GIPR antagonist 1 inhibits glucose-dependent insulinotropic polypeptide receptor signaling. GIPR antagonist 1 can be used for the research of type 2 diabetes and obesity.

HY-162433

GLP-1R agonist 41	Agonist
GLP-1R agonist 41 is an agonist for glucagon-like peptide-1 receptor (GLP-1 receptor), with EC₅₀ of 0.0187 nM.

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.

HY-13749S2

Sitagliptin-d₄	Inhibitor
Sitagliptin-d₄ (MK-0431-d₄) 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.

HY-P10952

Astepatide	Agonist
Astepatide is a gastric inhibitory peptide (GIP) receptor and glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in anti-diabetic research.

HY-P11275

TC4	Agonist
TC4 is a highly balanced single-molecule quadruple agonist that can respectively activate GIPR, GLP-1R, GcgR, and Y2R with IC₅₀ values of 0.95, 31, 81, and 1100 nM respectively. TC4 exhibits extremely strong signal bias on GLP-1R and has very low recruitment efficacy for β-inhibitor protein 2 (βArr2) and this strong cAMP preference is believed to maximize metabolic benefits (such as weight loss and hypoglycemia) while possibly minimizing side effects mediated by β-inhibitor protein recruitment (such as receptor desensitization). TC4 can be used for research on obesity and diabetes.

HY-118092

JWU-A021	Activator
JWU-A021 is a GLP-1 secretagogue with an EC₅₀ of 1.9 μM. JWU-A021 activates the TRPA1 cation channel to promote calcium ion influx and increase intracellular calcium levels in enteroendocrine cells and TRPA1-transfected cells. By activating the TRPA1 channel, JWU-A021 stimulates the secretion of GLP-1 from intestinal enteroendocrine cells and intestinal L cells. JWU-A021 is applicable to research related to type 2 diabetes.

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GLP Receptor

GLP Receptor Related Products (201)

Antibodies (1)

GLP Receptor Related Products (201):