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GIPR/GLP-1R agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	GLP Receptor (14) Antibody-Drug Conjugates (ADCs) (1) GCGR (9) Insulin Receptor (2) Neuropeptide Y Receptor (2)
By Research Areas:	Cardiovascular Disease (2) Inflammation/Immunology (2) Metabolic Disease (15)

Inhibitors & Agonists

Fluorescent Dyes

Peptides

Targets Recommended: GLP Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P3506

Retatrutide 3 Publications Verification LY3437943	GCGR GLP Receptor	Metabolic Disease
Retatrutide (LY3437943) is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide binds human GCGR, GIPR, and GLP-1R with EC₅₀ values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide can be used for the research of obesity .

HY-164535

Maridebart cafraglutide AMG 133	Antibody-Drug Conjugates (ADCs) GLP Receptor Insulin Receptor	Metabolic Disease
Maridebart cafraglutide (AMG 133) is a long-acting peptide-antibody conjugate that combines GLP-1 receptor agonist with glucose-dependent insulinotropic polypeptide (GIP) receptor antagonism. Maridebart cafraglutide shows antagonist activity against human, cynomolgus monkey and rat GIPR with IC₅₀ values of 46.4 nM, 26.5 nM, 822.3 nM, respectively. Maridebart cafraglutide shows agonist activity against human, cynomolgus monkey, rat and mouse GLP-1R with EC₅₀ values of 24.4 pM, 5.7 pM, 2.4 pM and 123 pM, respectively. Maridebart cafraglutide can be used for the study of obesity and type 2 diabetes .

HY-P3506A

Retatrutide TFA 3 Publications Verification LY3437943 TFA	GLP Receptor GCGR	Metabolic Disease
Retatrutide (LY3437943) TFA is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide TFA binds human GCGR, GIPR, and GLP-1R with EC₅₀ values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide TFA can be used for the research of obesity .

HY-P10736

AMG133 peptide payload	GCGR	Metabolic Disease
AMG133 peptide payload is a GLP-1 analog agonist peptide. AMG133 peptide potently activates GLP-1R, and exhibits weight loss and metabolic improvement activities. AMG133 peptide payload can be used for the synthesis of AMG 133 (HY-164535) .

HY-P10302A

GLP-1R/GIPR agonist-1 (soduim)	GLP Receptor	Metabolic Disease Inflammation/Immunology
GLP-1R/GIPR agonist-1 sodium is a dual *GLP-1/GIP* receptor agonist, with an EC₅₀ of 0.57 nM for *GLP-1R* and an EC₅₀ of 0.75 nM for *GIPR. GLP-1R/GIPR* agonist-1 sodium reduces food intake, inhibits weight gain, repairs islet damage, improves glucose tolerance, regulates serum lipid and liver enzyme levels, ameliorates hepatic vacuolization, reduces hepatic fat accumulation, delays the progression of hepatic fibrosis, and exhibits long-lasting hypoglycemic activity. GLP-1R/GIPR agonist-1 sodium can be used in research related to type 2 diabetes, obesity, and non-alcoholic steatohepatitis .

HY-P10031

SAR441255	GLP Receptor GCGR	Metabolic Disease
SAR441255 is a *GLP-1R/GCGR/GIPR* agonist, with human EC₅₀ values of 1.03 pM, 1.01 pM, and 0.73 pM, respectively. SAR441255 stimulates receptor activity and drives cAMP accumulation. SAR441255 can be used for the research of type 2 diabetes, obesity .

HY-P10302

GLP-1R/GIPR agonist-1	GLP Receptor Insulin Receptor	Metabolic Disease
GLP-1R/GIPR AgonIST-1 is a double-receptor agonist for *GLP-1* (glucagon-like peptide-1) and GIP (glucose-dependent insulin releasing peptide). GLP-1R/GIPR agonist-1 lowers blood sugar by mimicking the action of endogenous hormones *GLP-1* and GIP, enhancing insulin secretion while inhibiting glucagon secretion. GLP-1R/GIPR agonist-1 can be used in the study of metabolic diseases such as diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .

HY-P3506B

Retatrutide acetate LY3437943 acetate	GCGR GLP Receptor	Metabolic Disease
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 .

HY-173479

GLP-1R agonist 30	GLP Receptor	Cardiovascular Disease Metabolic Disease
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 .

HY-171302

GLP-1R/GIPR agonist-2	GLP Receptor	Metabolic Disease
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-P11279

TC2	GLP Receptor GCGR Neuropeptide Y Receptor	Metabolic Disease
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 .

HY-P11275

TC4	GLP Receptor GCGR Neuropeptide Y Receptor	Metabolic Disease
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-P11487

UTG-4	GLP Receptor GCGR	Cardiovascular Disease Metabolic Disease
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 (K_d = 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 .

HY-181709

TPM003 TG062	GLP Receptor GCGR	Metabolic Disease Inflammation/Immunology
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 .

HY-P11672

Poterepatide HDM1005	GLP Receptor	Metabolic Disease
Poterepatide (HDM1005) is a long-acting *GLP-1R/GIPR* peptide dual agonist. Poterepatide exhibits potent activity on both GLP-1 and GIP receptors. Poterepatide can be used for the study of obesity and type 2 diabetes .

Cat. No.	Product Name	Type

HY-164535

Maridebart cafraglutide AMG 133	Fluorescent Dyes
Maridebart cafraglutide (AMG 133) is a long-acting peptide-antibody conjugate that combines GLP-1 receptor agonist with glucose-dependent insulinotropic polypeptide (GIP) receptor antagonism. Maridebart cafraglutide shows antagonist activity against human, cynomolgus monkey and rat GIPR with IC₅₀ values of 46.4 nM, 26.5 nM, 822.3 nM, respectively. Maridebart cafraglutide shows agonist activity against human, cynomolgus monkey, rat and mouse GLP-1R with EC₅₀ values of 24.4 pM, 5.7 pM, 2.4 pM and 123 pM, respectively. Maridebart cafraglutide can be used for the study of obesity and type 2 diabetes .

Maridebart cafraglutide

AMG 133

Fluorescent Dyes

Maridebart cafraglutide (AMG 133) is a long-acting peptide-antibody conjugate that combines GLP-1 receptor agonist with glucose-dependent insulinotropic polypeptide (GIP) receptor antagonism. Maridebart cafraglutide shows antagonist activity against human, cynomolgus monkey and rat GIPR with IC₅₀ values of 46.4 nM, 26.5 nM, 822.3 nM, respectively. Maridebart cafraglutide shows agonist activity against human, cynomolgus monkey, rat and mouse GLP-1R with EC₅₀ values of 24.4 pM, 5.7 pM, 2.4 pM and 123 pM, respectively. Maridebart cafraglutide can be used for the study of obesity and type 2 diabetes .

Cat. No.	Product Name	Target	Research Area

HY-P3506

Retatrutide 3 Publications Verification LY3437943	GCGR GLP Receptor	Metabolic Disease
Retatrutide (LY3437943) is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide binds human GCGR, GIPR, and GLP-1R with EC₅₀ values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide can be used for the research of obesity .

HY-P3506A

Retatrutide TFA 3 Publications Verification LY3437943 TFA	GLP Receptor GCGR	Metabolic Disease
Retatrutide (LY3437943) TFA is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide TFA binds human GCGR, GIPR, and GLP-1R with EC₅₀ values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide TFA can be used for the research of obesity .

HY-P10736

AMG133 peptide payload	GCGR	Metabolic Disease
AMG133 peptide payload is a GLP-1 analog agonist peptide. AMG133 peptide potently activates GLP-1R, and exhibits weight loss and metabolic improvement activities. AMG133 peptide payload can be used for the synthesis of AMG 133 (HY-164535) .

HY-P10302A

GLP-1R/GIPR agonist-1 (soduim)	GLP Receptor	Metabolic Disease Inflammation/Immunology
GLP-1R/GIPR agonist-1 sodium is a dual *GLP-1/GIP* receptor agonist, with an EC₅₀ of 0.57 nM for *GLP-1R* and an EC₅₀ of 0.75 nM for *GIPR. GLP-1R/GIPR* agonist-1 sodium reduces food intake, inhibits weight gain, repairs islet damage, improves glucose tolerance, regulates serum lipid and liver enzyme levels, ameliorates hepatic vacuolization, reduces hepatic fat accumulation, delays the progression of hepatic fibrosis, and exhibits long-lasting hypoglycemic activity. GLP-1R/GIPR agonist-1 sodium can be used in research related to type 2 diabetes, obesity, and non-alcoholic steatohepatitis .

HY-P10031

SAR441255	GLP Receptor GCGR	Metabolic Disease
SAR441255 is a *GLP-1R/GCGR/GIPR* agonist, with human EC₅₀ values of 1.03 pM, 1.01 pM, and 0.73 pM, respectively. SAR441255 stimulates receptor activity and drives cAMP accumulation. SAR441255 can be used for the research of type 2 diabetes, obesity .

HY-P10302

GLP-1R/GIPR agonist-1	GLP Receptor Insulin Receptor	Metabolic Disease
GLP-1R/GIPR AgonIST-1 is a double-receptor agonist for *GLP-1* (glucagon-like peptide-1) and GIP (glucose-dependent insulin releasing peptide). GLP-1R/GIPR agonist-1 lowers blood sugar by mimicking the action of endogenous hormones *GLP-1* and GIP, enhancing insulin secretion while inhibiting glucagon secretion. GLP-1R/GIPR agonist-1 can be used in the study of metabolic diseases such as diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .

HY-P3506B

Retatrutide acetate LY3437943 acetate	GCGR GLP Receptor	Metabolic Disease
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 .

HY-P11279

TC2	GLP Receptor GCGR Neuropeptide Y Receptor	Metabolic Disease
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 .

HY-P11275

TC4	GLP Receptor GCGR Neuropeptide Y Receptor	Metabolic Disease
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-P11487

UTG-4	GLP Receptor GCGR	Cardiovascular Disease Metabolic Disease
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 (K_d = 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 .

HY-P11672

Poterepatide HDM1005	GLP Receptor	Metabolic Disease
Poterepatide (HDM1005) is a long-acting *GLP-1R/GIPR* peptide dual agonist. Poterepatide exhibits potent activity on both GLP-1 and GIP receptors. Poterepatide can be used for the study of obesity and type 2 diabetes .

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