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antagonism studies

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Antibody-Drug Conjugates (ADCs) (1) FXR (1) GLP Receptor (1) Insulin Receptor (1) Melanocortin Receptor (1) Opioid Receptor (1) Parasite (1)
By Research Areas:	Infection (1) Metabolic Disease (3) Neurological Disease (2)

Inhibitors & Agonists

Fluorescent Dyes

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-P10571

GPS1573	Melanocortin Receptor	Metabolic Disease
GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC₅₀=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .

HY-151481

FXR antagonist 1	FXR	Metabolic Disease
FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC₅₀=2.1 μM). FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies .

HY-159080

HgCht2-IN-1	Parasite	Infection
HgCht2-IN-1 (compound 1516b) is a HgCht2 inhibitor that successfully inhibits the antagonism of cyst nematodes against nitrogen-fixing rhizobia and phosphate-absorbing arbuscular mycorrhizal symbionts. HgCht2-IN-1 can be used in the study of cyst nematode antagonism against microbial symbionts .

HY-120810

MCI-225 hydrate hydrochloride DDP-225 hydrate hydrochloride	5-HT Receptor	Neurological Disease
MCI-225 (DDP-225) hydrate hydrochloride is a selective and orally active noradrenaline (NA) reuptake inhibitor with 5-HT3 receptor antagonism. MCI-225 hydrate hydrochloride has antidepressant-like and anxiolytic-like properties. MCI-225 hydrate hydrochloride can be used for the study of anxiety disorder .

HY-179282

Mu opioid receptor antagonist 9	Opioid Receptor	Neurological Disease
Mu opioid receptor antagonist 9 is potent, selective and CNS-pentrant mu-opioid receptor (MOR) antagonist with a K_i of 77.3 nM. Mu opioid receptor antagonist 9 exhibits selectivity over kappa-opioid receptor (KOR), and delta-opioid receptor (DOR). Mu opioid receptor antagonist 9 effectively blocks the antinociceptive effects of psychoactive substances. Mu opioid receptor antagonist 9 can reverse psychoactive substances-induced respiratory depression in mice. Mu opioid receptor antagonist 9 can be used for the research of Opioid Use Disorder (OUD) .

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-P10571

GPS1573	Melanocortin Receptor	Metabolic Disease
GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC₅₀=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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