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Results for "

CCK antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Cholecystokinin Receptor (54) Akt (3) CCR (1) Drug Isomer (1) Endogenous Metabolite (1) Ephrin Receptor (3) HIF/HIF Prolyl-Hydroxylase (3) Histone Methyltransferase (1) Interleukin Related (3) P-glycoprotein (2) Reference Standards (2) VEGFR (3)
By Research Areas:	Cancer (15) Endocrinology (16) Inflammation/Immunology (6) Metabolic Disease (22) Neurological Disease (24)

Inhibitors & Agonists

Peptides

Targets Recommended: Cholecystokinin Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-162070

CCK antagonist 1	Cholecystokinin Receptor	Neurological Disease Cancer
CCK antagonist 1 (compound 3d) is a *CCK* antagonist with IC₅₀s of 1.1 μM and 4 μM for CCK1 and CCK2, respectively. CCK antagonist 1 can be used for research of cancer and mental disease .

HY-129357

CCK-B Receptor Antagonist 2	Cholecystokinin Receptor	Metabolic Disease
CCK-B Receptor Antagonist 2, compound 15b, is a potent and orally active *Gastrin/CCK-B* antagonist with an IC₅₀ value of 0.43 nM. CCK-B Receptor Antagonist 2 also inhibits gastrin/CCK-A activity with an IC₅₀ of 1.82 μM .

HY-B2154

Loxiglumide 4 Publications Verification CR-1505	Cholecystokinin Receptor	Metabolic Disease Endocrinology
Loxiglumide is a cholecystokinin (CCK-1) receptor antagonist.

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-U00375

*Gastrin/CCK* antagonist 1**	Cholecystokinin Receptor	Endocrinology
Gastrin/CCK antagonist 1 is an antagonist of *gastrin/CCK*, used for the research of gastrointestinal disorders.

HY-P2638

Cholecystokinin (27-32)-amide CCK-27-32-NH2	Cholecystokinin Receptor	Neurological Disease
Cholecystokinin (27-32)-amide (CCK-27-32-NH2) is a potent cholecystokinin receptor *CCK* receptor antagonist .

HY-P2165

N-acetyl CCK-(26-30) amide CCK-(26-30) (sulfated)	Cholecystokinin Receptor	Neurological Disease
N-acetyl CCK-(26-30) amide (CCK-(26-30) (sulfated)) is a *cholecystokinin (CCK) receptor* antagonist .

HY-118546

JNJ-17156516	Cholecystokinin Receptor	Inflammation/Immunology
JNJ-17156516 is an orally active, potent, and selective cholecystokinin (CCK)1-receptor antagonist .

HY-116576

LY219057	Cholecystokinin Receptor	Metabolic Disease
LY219057 is a potent antagonist of cholecystokinin octapeptide (CCK-8), with the ID₅₀ of 287.5 nM .

HY-P2055

A-57696	Endogenous Metabolite	Endocrinology
A-57696 is a cholecystokinin antagonist with selective activity at cortical CCK-B receptors (IC50 = 25 nM). A-57696 behaves as a competitive antagonist in reversing CCK8-stimulated pancreatic alpha-amylase secretion and phosphatidylinositol degradation. A-57696 fails to induce gallbladder contraction and inhibits CCK8-induced contraction. A-57696 behaves as a partial agonist at CCK-B/gastrin receptors on NCI-H345 cells, achieving 80% of the maximal CCK8 response. A-57696 and CCK8 inhibit each other in a calcium mobilization assay .

HY-U00062

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

HY-118904

VL-0395	Cholecystokinin Receptor	Metabolic Disease
VL-0395 is a *CCK1* selective antagonist with IC₅₀ of 0.197 μM for *CCK1* in rat pancreatic acinar cells .

HY-118314

CI-1015 PD 144598	Cholecystokinin Receptor	Cancer
CI-1015 is a potent CCK-B receptor antagonist.

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-19261

T-0632	Cholecystokinin Receptor	Metabolic Disease
T-0632 is a CCK A receptor antagonist that exhibits significant pharmacological properties in in vitro studies. T-0632 competitively inhibits the binding of [125I]CCK-8 to rat pancreatic CCK A receptors with a K_i value of 0.24 nM, which is significantly lower than the K_i value for guinea pig CCK B receptors. T-0632 has higher selectivity in inhibiting CCK-8-stimulated pancreatic enzyme release, with an IC_50 value of 5.0 nM, which is more advantageous than L-364,718 and loxiglumide. In rabbit gallbladder smooth muscle, the antagonistic effects of T-0632 and loxiglumide are reversible, while L-364,718 shows a persistent inhibitory effect. These results indicate that T-0632 is a highly potent, reversible and more selective CCK A receptor antagonist.

HY-B1439B

Lorglumide sodium salt CR-1409 sodium salt	Cholecystokinin Receptor	Metabolic Disease Endocrinology
Lorglumide sodium salt (CR-1409 sodium salt) is a potent cholecystokinin (CCK) receptor antagonist .

HY-105226B

CI-988 hemihydrate PD134308 hemihydrate	Cholecystokinin Receptor	Neurological Disease Cancer
CI-988 hemihydrate (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC₅₀ of 1.7 nM for mouse cortex CCK2. CI-988 hemihydrate shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 hemihydrate has anxiolytic and anti-tumor effects .

HY-105226

CI-988 PD134308	Cholecystokinin Receptor	Neurological Disease Cancer
CI-988 (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC₅₀ of 1.7 nM for mouse cortex CCK2. CI-988 shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 has anxiolytic and anti-tumor effects .

HY-19445

Gastrazole JB95008	Cholecystokinin Receptor	Cancer
Gastrazole (JB95008) is potent and selective CCK2/gastrin receptor antagonist. Gastrazole can decrease the level of gastric acid. Gastrazole inhibits the Gastrin-stimulated growth of pancreatic cancer .

HY-103354

Proglumide sodium 2 Publications Verification	Cholecystokinin Receptor	Neurological Disease Endocrinology Cancer
Proglumide sodium is a nonpeptide and orally active *cholecystokinin (CCK)-A/B receptors* antagonist. Proglumide sodium selective blocks *CCK*’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities .

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-B1330

Proglumide 2 Publications Verification	Cholecystokinin Receptor	Neurological Disease Endocrinology Cancer
Proglumide is a nonpeptide and orally active *cholecystokinin (CCK)-A/B receptors* antagonist. Proglumide selective blocks *CCK*’s effects in the central nervous system (CNS). Proglumide has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide also has antiepileptic and antioxidant activities .

HY-100481

RP 72540 RPR101048	Cholecystokinin Receptor	Neurological Disease
RP 72540 is a selective *CCK-B* receptor antagonist, with IC₅₀ values of 2.4, 1.2, and 3.8 nM for *CCK-B* receptors in the guinea pig cerebral cortex, rat cerebral cortex, and mouse brain, respectively. RP 72540 effectively inhibits *CCK-8*-induced neuronal firing and dose-dependently inhibits gastric acid secretion, making it potentially valuable in studies of acid secretion. RP 72540 is an important tool for investigating the physiological functions of CCK B receptors .

HY-103354A

Proglumide hemicalcium	Cholecystokinin Receptor	Neurological Disease Endocrinology Cancer
Proglumide hemicalcium is a nonpeptide and orally active *cholecystokinin (CCK)-A/B receptors* antagonist. Proglumide hemicalcium selective blocks *CCK*’s effects in the central nervous system (CNS). Proglumide hemicalcium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide hemicalcium also has antiepileptic and antioxidant activities .

HY-U00360R

(Rac)-Sograzepide (Standard)	Cholecystokinin Receptor	Metabolic Disease
(Rac)-Sograzepide is an antagonist of cholecystokinin B (CCK-B) receptor, and has the potential of reducing the secretion of gastric acid.

HY-U00360

(Rac)-Sograzepide (Rac)-Netazepide; (Rac)-YF 476; (Rac)-YM-220	Cholecystokinin Receptor	Metabolic Disease
(Rac)-Sograzepide is an antagonist of cholecystokinin B *(CCK-B) receptor*, and has the potential of reducing the secretion of gastric acid.

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-P1988

JMV 179	Cholecystokinin Receptor	Metabolic Disease
JMV 179, a peptide closely related to CCK, is a cholecystokinin receptor (CKK) antagonist, with an IC₅₀ of 30 nM .

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-P2121

JMV 176	Cholecystokinin Receptor	Neurological Disease
Jmv 176 is a *CCK* agonist when first given and becomes a cholecystokinin antagonist after 3-4 hours .

HY-103354R

Proglumide sodium (Standard)	Reference Standards Cholecystokinin Receptor	Neurological Disease Endocrinology Cancer
Proglumide (sodium) (Standard) is the analytical standard of Proglumide (sodium). This product is intended for research and analytical applications. Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities .

HY-B1330R

Proglumide (Standard)	Cholecystokinin Receptor	Neurological Disease Endocrinology Cancer
Proglumide (Standard) is the analytical standard of Proglumide. This product is intended for research and analytical applications. Proglumide is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide selective blocks CCK’s effects in the central nervous system (CNS). Proglumide has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide also has antiepileptic and antioxidant activities .

HY-106356

GV-150013	Cholecystokinin Receptor	Others
GV-150013 is a selective *CCK-B* receptor antagonist. GV-150013 has sleep aid effect .

HY-101764

Lintitript SR 27897	Cholecystokinin Receptor	Metabolic Disease
Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide *cholecystokinin (CCK1) receptor* antagonist with an EC₅₀ of 6 nM and a K_i of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for *CCK1* than CCK2 receptors (EC₅₀ value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin .

HY-14850

Sograzepide Netazepide; YF 476; YM-220	Cholecystokinin Receptor	Metabolic Disease Endocrinology
Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent, highly selective and orally active *Gastrin/CCK-B* antagonist with an IC₅₀ value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC₅₀ of 502 nM . Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with K_i values of 0.068, 0.62 and 0.19 nM, respectively .

HY-111313

JNJ-26070109	Cholecystokinin Receptor	Metabolic Disease
JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pK_is of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. The dual function of CCK2 receptors in regulating gastric acid secretion and growth of the gastrointestinal mucosa make this an attractive and novel target for the research of gastroesophageal reflux disease .

HY-121278

Benzotript Benzotriptum	Cholecystokinin Receptor	Inflammation/Immunology Cancer
Benzotript (Benzotriptum) is a cholecystokinin-receptor (CCK) and gastrin receptor antagonist. Benzotript shows antiproliferative effects in human colon carcinoma cell lines .

HY-101352

LY 225910	Cholecystokinin Receptor	Neurological Disease
LY 225910 is a selective antagonist for cholecystokinin receptor (CCK2 receptor), which affects the excitatory response to morphine, and leads to morphine sensitization .

HY-106840A

L-365260 hemihydrate 1 Publications Verification	Cholecystokinin Receptor	Neurological Disease Metabolic Disease
L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with K_is of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors .

HY-148656

PNB-001	Cholecystokinin Receptor	Inflammation/Immunology
PNB-001 is an orally active *CCK2* selective ligand and antagonist. PNB-001 has anti-inflammatory and analgesic activities .

HY-B1439BR

Lorglumide sodium salt (Standard)	Cholecystokinin Receptor	Metabolic Disease Endocrinology
Lorglumide sodium salt (Standard) is the analytical standard of Lorglumide sodium salt. This product is intended for research and analytical applications. Lorglumide sodium salt (CR-1409 sodium salt) is a potent cholecystokinin (CCK) receptor antagonist .

HY-106301

Devazepide 4 Publications Verification L-364,718; MK-329	Cholecystokinin Receptor	Metabolic Disease
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of *cholecystokinin (CCK) receptor, with IC₅₀s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK* receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .

HY-17617

Nastorazepide Z-360	Cholecystokinin Receptor Ephrin Receptor Interleukin Related VEGFR HIF/HIF Prolyl-Hydroxylase Akt	Neurological Disease Cancer
Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and *gastrin/CCK-2* receptor antagonist. Nastorazepide inhibits the specific binding of [ ³H]CCK-8 to the human CCK-2 receptor with a K_i value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain .

HY-103357

LY288513	Cholecystokinin Receptor	Neurological Disease
LY288513 is a selective non-peptide *CCK-B* receptor antagonist with an IC₅₀ value of 16 nM. LY288513 produces an anxiolytic-like action in mice .

HY-125610

DA-3934	Cholecystokinin Receptor	Neurological Disease
DA-3934 is a *cholecystokinin (CCK)-B receptor* antagonist. DA-3934 inhibits Pentagastrin (HY-A0261)-induced gastric acid secretion in rats .

HY-129759

KSG-504 anhydrous	Cholecystokinin Receptor	Inflammation/Immunology
KSG-504 (anhydrous) is a CCK receptor antagonist. KSG-504 (anhydrous) inhibits the development of Ethionine-induced acute pancreatitis in rats and facilitates the regeneration of acinar cells .

HY-14575

Nastorazepide hemicalcium Z-360 hemicalcium	Cholecystokinin Receptor Ephrin Receptor Interleukin Related VEGFR HIF/HIF Prolyl-Hydroxylase Akt	Neurological Disease Cancer
Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and *gastrin/CCK-2* receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [ ³H]CCK-8 to the human CCK-2 receptor with a K_i value of 0.47 nM. Nastorazepide hemicalcium inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer. Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain .

HY-106840

L-365260 1 Publications Verification	Cholecystokinin Receptor	Neurological Disease Metabolic Disease
L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with K_is of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance .

HY-103357A

LY262691	Cholecystokinin Receptor	Neurological Disease
LY262691 is a selective *CCK-B* antagonist with antipsychotic properties. LY262691 decreases the number of spontaneously active A9 and A10 dopamine cells and can be utilized in antipsychotic research .

HY-17617R

Nastorazepide (Standard)	Cholecystokinin Receptor Ephrin Receptor Interleukin Related VEGFR HIF/HIF Prolyl-Hydroxylase Akt	Neurological Disease Cancer
Nastorazepide (Standard) is the analytical standard of Nastorazepide. This product is intended for research and analytical applications. Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain .

Cat. No.	Product Name	Target	Research Area

HY-P2638

Cholecystokinin (27-32)-amide CCK-27-32-NH2	Cholecystokinin Receptor	Neurological Disease
Cholecystokinin (27-32)-amide (CCK-27-32-NH2) is a potent cholecystokinin receptor *CCK* receptor antagonist .

HY-P2165

N-acetyl CCK-(26-30) amide CCK-(26-30) (sulfated)	Cholecystokinin Receptor	Neurological Disease
N-acetyl CCK-(26-30) amide (CCK-(26-30) (sulfated)) is a *cholecystokinin (CCK) receptor* antagonist .

HY-P2055

A-57696	Endogenous Metabolite	Endocrinology
A-57696 is a cholecystokinin antagonist with selective activity at cortical CCK-B receptors (IC50 = 25 nM). A-57696 behaves as a competitive antagonist in reversing CCK8-stimulated pancreatic alpha-amylase secretion and phosphatidylinositol degradation. A-57696 fails to induce gallbladder contraction and inhibits CCK8-induced contraction. A-57696 behaves as a partial agonist at CCK-B/gastrin receptors on NCI-H345 cells, achieving 80% of the maximal CCK8 response. A-57696 and CCK8 inhibit each other in a calcium mobilization assay .

HY-P1988

JMV 179	Cholecystokinin Receptor	Metabolic Disease
JMV 179, a peptide closely related to CCK, is a cholecystokinin receptor (CKK) antagonist, with an IC₅₀ of 30 nM .

HY-P2121

JMV 176	Cholecystokinin Receptor	Neurological Disease
Jmv 176 is a *CCK* agonist when first given and becomes a cholecystokinin antagonist after 3-4 hours .

HY-P2025

JMV 236	Histone Methyltransferase	Neurological Disease
JMV 236 is a cholecystokinin antagonist with appetite-suppressing activity. JMV 236 affects the regulation of food intake through the interaction of the intestinal endogenous peptide PrRP and the CCK1 receptor. The administration of JMV 236 activates PrRP neurons located in the NTS, thereby enhancing its appetite-suppressing effect. JMV 236 has significant effects on areas of the central nervous system associated with food intake, especially during states of starvation .

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