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CCK-A receptors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Cholecystokinin Receptor (15) CCR (2) Drug Isomer (1) NO Synthase (1) P-glycoprotein (2) Reference Standards (2) Sigma Receptor (1)
By Research Areas:	Cardiovascular Disease (1) Endocrinology (6) Inflammation/Immunology (3) Metabolic Disease (11) Neurological Disease (4)

Inhibitors & Agonists

Peptides

Targets Recommended: Cholecystokinin Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-128878

Dexloxiglumide	Cholecystokinin Receptor P-glycoprotein	Metabolic Disease Endocrinology
Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide is the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). Dexloxiglumide exhibits moderate Caco-2 permeability that is polarized, concentration dependent, and pH dependent. Dexloxiglumide increases MRP1-substrate fluorescein uptake. Dexloxiglumide can be studied in research for gastrointestinal diseases and tumors .

HY-103355

YM022 2 Publications Verification	CCR	Metabolic Disease
YM022 is a highly potent, selective and orally active *gastrin/cholecystokinin (CCK)-B receptor* (CCK-BR) antagonist. YM022 shows the K_i** values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively . YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo .

HY-118194

A-65186	Cholecystokinin Receptor	Others
A-65186 is a CCK-A receptor antagonist with the activity of inhibiting CCK8-induced amylase secretion. A-65186 has high binding affinity for pancreatic CCK-A receptors, is more than 500 times more selective for CCK-A receptors than for CCK-B receptors, and can inhibit CCK8-induced amylase secretion.

HY-123434

PD-149164	Cholecystokinin Receptor	Metabolic Disease Endocrinology
PD-149164 is a potent agonist of cholecystokinin B (CCK-B) receptor, with IC₅₀ values of 0.083 nM and 75 nM in binding assay to CCK-B and CCK-A .

HY-U00363

CHEMBL333994 FK-480	Cholecystokinin Receptor	Endocrinology
CHEMBL333994 (FK-480) is a potent and orally active Cholecystokinin A receptor (CCK-A receptor) antagonist, with an IC₅₀ of 0.67 nM. CHEMBL333994 selectively antagonizes peripheral CCK receptors. CHEMBL333994 increases CCK mRNA level. CHEMBL333994 can be used for research of chronic pancreatitis .

HY-U00062

Tarazepide	Cholecystokinin Receptor	Metabolic Disease Endocrinology
Tarazepide is a potent and specific *CCK-A* receptor antagonist.

HY-111918

A71378	Cholecystokinin Receptor	Metabolic Disease
A71378 is a selectivity **CCK-A receptor agonist the IC₅₀** values of 0.4 nM, 300 nM, and 1,200 nM for the pancreatic CCK-A, cortical CCK-B, and gastrin receptor, respectively. A71378 elicits pancreatic amylase secretion (EC₅₀ = 0.16 nM) and ileal muscle contraction (EC₅₀ = 3.7 nM) .

HY-U00387

CCK-A receptor inhibitor 1	Cholecystokinin Receptor	Metabolic Disease Endocrinology
CCK-A receptor inhibitor 1 is a cholecystokinin A (CCK-A) *receptor* inhibitor with a binging IC₅₀ of 340 nM.

HY-123182

PD-140548	Cholecystokinin Receptor	Neurological Disease
PD-140548 is a selective cholecystokinin (CCKA) receptor antagonist. PD-140548 can be used in schizophrenia research .

HY-119127

TP-680	Cholecystokinin Receptor	Metabolic Disease
TP-680 is a cholecystokinin receptor antagonist. TP-680 binds 1510 times more strongly to rat pancreatic *CCK_A* receptors (IC₅₀=1.2 nM) than to rat brain CCK_B receptors (IC₅₀=1812.5 nM). TP-680 can be used in the study of gastrointestinal diseases .

HY-U00363A

(rac)-CHEMBL333994 (rac)-FK-480	Cholecystokinin Receptor Drug Isomer	Inflammation/Immunology
(rac)-CHEMBL333994 is the racemate of CHEMBL333994 (HY-U00363). CHEMBL333994 is a potent and orally active Cholecystokinin A receptor (CCK-A receptor) antagonist, with an IC₅₀ of 0.67 nM. CHEMBL333994 selectively antagonizes peripheral CCK receptors. CHEMBL333994 increases CCK mRNA level. CHEMBL333994 can be used for research of chronic pancreatitis .

HY-129516

A-70874	Cholecystokinin Receptor	Metabolic Disease
A-70874 is a tyrosine-free tetrapeptide analog of cholecystokinin (30-33) (CCK-4). A-70874 is an agonist that stimulates pancreatic amylase release and a partial agonist that stimulates pancreatic phosphoinositide decomposition. A-70874 has an IC₅₀ of 4.9 nM for the guinea pig pancreatic CCK receptor. Cholecystokinin (CCK) receptors are divided into CCK-A (digestive tract) and CCK-B (brain). A-70874 has an affinity of 1.6 μM for the CCK-B/gastrin receptor .

HY-118665

L-736380	Cholecystokinin Receptor	Metabolic Disease
L-736380 is a high affinity CCK-B (cholecystokinin B receptor) receptor antagonist, with IC₅₀ values of 0.054 nM and 400 nM for CCK-B and CCK-A, respectively. L-736380 dose-dependently inhibits gastric acid secretion in anesthetized rats (ID₅₀, 0.064 mg/kg) and ex vivo binding of [125I]CCK-8S in BKTO mice brain membranes (ED₅₀, 1.7 mg/kg) .

HY-128878R

Dexloxiglumide (Standard)	Cholecystokinin Receptor P-glycoprotein Reference Standards	Metabolic Disease Endocrinology
Dexloxiglumide (Standard) is the analytical standard of Dexloxiglumide. This product is intended for research and analytical applications. Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide is the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). Dexloxiglumide exhibits moderate Caco-2 permeability that is polarized, concentration dependent, and pH dependent. Dexloxiglumide increases MRP1-substrate fluorescein uptake. Dexloxiglumide can be studied in research for gastrointestinal diseases and tumors .

HY-108515

(+)-Igmesine hydrochloride JO1784	Sigma Receptor NO Synthase	Cardiovascular Disease Neurological Disease Inflammation/Immunology
(+)-Igmesine hydrochloride (JO1784) is an orally active and selective σ₁ receptor ligand with an IC₅₀ of 39 nM. (+)-Igmesine hydrochloride binds σ₁ receptors to activate G-proteins and modulate Ca ²⁺ uptake. (+)-Igmesine (hydrochloride) attenuates ischaemia-induced nitric oxide synthase activity and hyperactivity. (+)-Igmesine hydrochloride can be used for the research of duodenal ulcers, gastric ulcers, and cerebral ischaemia .

HY-P1994A

JMV 170	Cholecystokinin Receptor	Neurological Disease
JMV 170, a CCK derivative, is a selective CCK-B agonist. JMV 170 binds to the CCK-B receptor with a 10-fold higher affinity than to the *CCK-A* receptor. JMV 170 shows contractile effects on pig smooth muscle cells with an EC₅₀ of 9 pmol/L .

HY-103355R

YM022 (Standard)	Reference Standards CCR	Metabolic Disease
YM022 (Standard) is the analytical standard of YM022 (HY-103355). This product is intended for research and analytical applications. YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the K_i values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively . YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo .

HY-116260

RP-69758	Cholecystokinin Receptor	Neurological Disease Inflammation/Immunology
RP-69758 is a potent and selective non-peptide cholecystokinin-B (CCK_B)/gastrin receptor antagonist. RP-69758 exhibits >200-fold selectivity for CCK_B over CCK_A receptors. RP-69758 antagonizes CCK-8-induced neuronal firing in rat hippocampal slices. RP-69758 inhibits Pentagastrin (HY-A0261)-induced gastric acid secretion in the rat. RP-69758 can be used for neurological disorders and gastrointestinal disease research .

Cat. No.	Product Name	Target	Research Area

HY-P1994A

JMV 170	Cholecystokinin Receptor	Neurological Disease
JMV 170, a CCK derivative, is a selective CCK-B agonist. JMV 170 binds to the CCK-B receptor with a 10-fold higher affinity than to the *CCK-A* receptor. JMV 170 shows contractile effects on pig smooth muscle cells with an EC₅₀ of 9 pmol/L .

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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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