Cholecystokinin Receptor Antagonist

Cholecystokinin Receptor Antagonists (48):

Cat. No.	Product Name	Effect	Purity

HY-106301

Devazepide	Antagonist	99.58%
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-155205

GV150013X	Antagonist
GV150013X is an antagonist for cholecystokinin-2/gastrin receptor (CCK2R), with K_i of 2.29 nM. GV150013X attenuates central nervous disorders, such as anxiety and panic disorder.

HY-100481

RP 72540	Antagonist
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-114966

RP73870	Antagonist
RP73870 is an orally active gastrin/cholecystokinin-B receptor antagonist. RP73870 inhibits basal gastric acid secretion in the rat. RP73870 has potent anti-ulcer activity.

HY-14850

Sograzepide	Antagonist	98.35%
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-106840

L-365260	Antagonist	99.93%
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-103354

Proglumide sodium	Antagonist	99.85%
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-B1330

Proglumide	Antagonist	99.74%
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-17617

Nastorazepide	Antagonist	99.95%
Nastorazepide (Z-360) is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity.

HY-128878

Dexloxiglumide	Antagonist	98.25%
Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide, the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8).

HY-101764

Lintitript	Antagonist	99.58%
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-B1439B

Lorglumide sodium salt	Antagonist	99.19%
Lorglumide sodium salt (CR-1409 sodium salt) is a potent cholecystokinin (CCK) receptor antagonist.

HY-B2154

Loxiglumide	Antagonist	≥98.0%
Loxiglumide is a cholecystokinin (CCK-1) receptor antagonist.

HY-148656

PNB-001	Antagonist	99.65%
PNB-001 is an orally active CCK2 selective ligand and antagonist. PNB-001 has anti-inflammatory and analgesic activities.

HY-106840A

L-365260 hemihydrate	Antagonist	99.75%
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-U00360

(Rac)-Sograzepide	Antagonist	98.98%
(Rac)-Sograzepide is an antagonist of cholecystokinin B (CCK-B) receptor, and has the potential of reducing the secretion of gastric acid.

HY-105226B

CI-988 hemihydrate	Antagonist
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-U00062

Tarazepide	Antagonist
Tarazepide is a potent and specific CCK-A receptor antagonist.

HY-19445

Gastrazole	Antagonist
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-150036

Anthramycin	Antagonist
Anthramycin, a member of the pyrolobenzodiazepine (PBD) family, is a potent antibiotic. Anthramycin has potent antitumor activity. Anthramycin can act as an potent antagonist of cholecystokinin in the central nervous system in mice.

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