Search Result
Results for "
Cholecystokinin Receptor
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P2932A
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Cholecystokinin Receptor
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Neurological Disease
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Cholecystokinin-33 free acid is an analogue of Cholecystokinin (HY-P2932). C-terminal amidation is important for binding of Cholecystokinin to its receptors, and removing the amide group would decrease Cholecystokinin activity. Cholecystokinin-33 free acid can be used to study C-terminal amidation of Cholecystokinin-33 .
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- HY-105257
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- HY-B2154
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- HY-128878
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Cholecystokinin Receptor
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Metabolic Disease
Endocrinology
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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) .
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- HY-125692
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- HY-P2199
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- HY-P2638
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- HY-U00387
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- HY-11076
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- HY-P1994
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- HY-B1439B
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- HY-155205
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Cholecystokinin Receptor
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Neurological Disease
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GV150013X is an antagonist for cholecystokinin-2/gastrin receptor (CCK2R), with Ki of 2.29 nM. GV150013X attenuates central nervous disorders, such as anxiety and panic disorder .
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- HY-118546
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- HY-120862
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- HY-169139
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- HY-11077
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- HY-125556
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Cholecystokinin tetrapeptide; CCK-4
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Cholecystokinin Receptor
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Metabolic Disease
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Tetragastrin (Cholecystokinin tetrapeptide; CCK-4) is the C-terminal tetrapeptide of gastrin. Tetragastrin can stimulate gastric secretion . Tetragastrin is a Cholecystokinin (CCK-4) receptor agonist . Gastric mucosal protection .
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- HY-U00360
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(Rac)-Netazepide; (Rac)-YF 476; (Rac)-YM-220
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Cholecystokinin Receptor
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Metabolic Disease
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(Rac)-Sograzepide is an antagonist of cholecystokinin B (CCK-B) receptor, and has the potential of reducing the secretion of gastric acid.
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- HY-121278
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- HY-101352
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- HY-P1988
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- HY-123182
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- HY-P1097
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- HY-P2165
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- HY-A0190
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- HY-158722
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- HY-129516
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Cholecystokinin Receptor
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Metabolic Disease
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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 .
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- HY-123434
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- HY-P2671
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Cholecystokinin Receptor
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Cancer
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[Leu15]-Gastrin I (human) is a Gastrin I, human (HY-P1097) peptide hormone derivative, which is trophic for normal gastrointestinal epithelium. Gastrin stimulates growth of gastric adenocarcinoma (gastric cancer) through G-protein-coupled receptor called the cholecystokinin (CCK) or cholecystokinin-B receptors (CCK-BR) that are overexpressed in this malignancy. [Leu15]-Gastrin I (human) is promising for research of gastric cancer .
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- HY-125610
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- HY-114966
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- HY-119127
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Cholecystokinin Receptor
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Metabolic Disease
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TP-680 is a cholecystokinin receptor antagonist. TP-680 binds 1510 times more strongly to rat pancreatic CCKA receptors (IC50=1.2 nM) than to rat brain CCKB receptors (IC50=1812.5 nM). TP-680 can be used in the study of gastrointestinal diseases .
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- HY-117839
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Cholecystokinin Receptor
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Neurological Disease
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PD-135666 is a dipeptide inhibitor of cholecystokinin B (CCK B) receptors, binding to CCK B receptors in mouse cerebral cortex with IC50 of 0.1 nM. Its enantiomer, PD-140548, preferentially binds to CCK A receptors with IC50 of 2.8 nM in rat pancreas. PD-135666 exhibits anxiolytic effects in animal models .
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- HY-106347
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CR 2945
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Cholecystokinin Receptor
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Inflammation/Immunology
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Itriglumide (CR 2945) is an anthranilic acid derivative. Itriglumide is a potent and selective CCKB receptor antagonist, with an IC50 of 2.3 nM. Itriglumide antagonizes the response to gastrin in a dose-dependent manner with an IC50 of 5.9 nM. Itriglumide shows antisecretory and antiulcer activity .
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- HY-106840A
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Cholecystokinin Receptor
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Neurological Disease
Metabolic Disease
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L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis 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 .
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- HY-P1537
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Neuropeptide Y Receptor
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Metabolic Disease
Endocrinology
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Pancreatic Polypeptide, bovine, a 36-amino acid, straight chain polypeptide derived primarily from the pancreas, inhibits secretin- and cholecystokinin-stimulated pancreatic secretion; Pancreatic Polypeptide, bovine acts as an agonist of NPY receptor, with high affinity at NPYR4.
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- HY-103355
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YM022
2 Publications Verification
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CCR
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Metabolic Disease
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YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki 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 .
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- HY-106301
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L-364,718; MK-329
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Cholecystokinin Receptor
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Metabolic Disease
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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 .
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- HY-A0261
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ICI-50123
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Cholecystokinin Receptor
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Endocrinology
Cancer
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Pentagastrin (ICI-50123) is a potent, selective Cholecystokinin B (CCKB) receptor antagonists with IC50 values of 11 nM and 1100 nM for CCKB and CCKA, respectively. Pentagastrin enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury . .
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- HY-160045
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Cholecystokinin Receptor
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Cancer
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AP1153 aptamer sodium is a DNA aptamer that specifically binds to the cholecystokinin receptor CCKBR (Kd: ~15 pM), but does not activate CCKBR-related signaling pathways. AP1153 aptamer sodium is internalized by pancreatic ductal adenocarcinoma (PDAC) cells in a receptor-mediated manner. AP1153 aptamer sodium can bioconjugate to the surface of fluorescent nanoparticles to facilitate nanoparticle delivery to PDAC tumors in vivo .
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- HY-A0261A
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ICI-50123 meglumine
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Cholecystokinin Receptor
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Endocrinology
Cancer
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Pentagastrin (ICI-50123) meglumine is a potent, selective Cholecystokinin B (CCKB) receptor antagonists with IC50 values of 11 nM and 1100 nM for CCKB and CCKA, respectively. Pentagastrin meglumine enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury . .
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- HY-125314
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Cholecystokinin Receptor
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Endocrinology
Cancer
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AG-041R is a potent and selective CCK2 Receptor/Gastrin antagonist. AG-041R inhibits gastrin-evoked secretion of pancreastatin with an IC50 of 2.2 nM. AG-041R inhibits cell growth of Mastomys ECL carcinoid tumor cells .
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- HY-111313
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Cholecystokinin Receptor
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Metabolic Disease
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JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pKis 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 .
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- HY-105226
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PD134308
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Cholecystokinin Receptor
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Neurological Disease
Cancer
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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 .
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- HY-106840
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Cholecystokinin Receptor
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Neurological Disease
Metabolic Disease
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L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis 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 .
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- HY-105226B
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PD134308 hemihydrate
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Cholecystokinin Receptor
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Neurological Disease
Cancer
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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 .
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- HY-103354
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Cholecystokinin Receptor
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Neurological Disease
Endocrinology
Cancer
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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 .
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- HY-B1330
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Cholecystokinin Receptor
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Neurological Disease
Endocrinology
Cancer
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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 .
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- HY-101764
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SR 27897
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Cholecystokinin Receptor
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Metabolic Disease
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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 Ki 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 .
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- HY-106301R
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Cholecystokinin Receptor
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Metabolic Disease
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Devazepide (Standard) is the analytical standard of Devazepide. This product is intended for research and analytical applications. 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 .
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- HY-103354A
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Cholecystokinin Receptor
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Neurological Disease
Endocrinology
Cancer
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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 .
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- HY-118665
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Cholecystokinin Receptor
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Metabolic Disease
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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) .
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- HY-169914
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JO 1784 hydrochloride
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Sigma Receptor
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Neurological Disease
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Igmesine hydrochloride (JO 1784) is an orally active σ-receptor ligand capable of blocking the increase in colonic electromechanical activity induced by emotional stress. Igmesine hydrochloride also eliminates the colonic motility stimulation induced by dopamine, as well as the stimulation induced by centrally injected D1 or D2 receptor agonists. Furthermore, Igmesine hydrochloride can block the colonic motility responses induced by corticotropin-releasing factor (CRF) and ES through central cholecystokinin (CCK) release and/or activation of supraspinal CCK pathways .
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- HY-103354R
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Cholecystokinin Receptor
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Neurological Disease
Endocrinology
Cancer
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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 .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P2932A
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Cholecystokinin Receptor
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Neurological Disease
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Cholecystokinin-33 free acid is an analogue of Cholecystokinin (HY-P2932). C-terminal amidation is important for binding of Cholecystokinin to its receptors, and removing the amide group would decrease Cholecystokinin activity. Cholecystokinin-33 free acid can be used to study C-terminal amidation of Cholecystokinin-33 .
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- HY-125556
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Cholecystokinin tetrapeptide; CCK-4
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Cholecystokinin Receptor
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Metabolic Disease
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Tetragastrin (Cholecystokinin tetrapeptide; CCK-4) is the C-terminal tetrapeptide of gastrin. Tetragastrin can stimulate gastric secretion . Tetragastrin is a Cholecystokinin (CCK-4) receptor agonist . Gastric mucosal protection .
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- HY-P1097
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- HY-A0190
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- HY-P2199
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- HY-P2638
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- HY-P1994
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- HY-P1988
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- HY-P2165
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- HY-158722
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- HY-P2671
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Cholecystokinin Receptor
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Cancer
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[Leu15]-Gastrin I (human) is a Gastrin I, human (HY-P1097) peptide hormone derivative, which is trophic for normal gastrointestinal epithelium. Gastrin stimulates growth of gastric adenocarcinoma (gastric cancer) through G-protein-coupled receptor called the cholecystokinin (CCK) or cholecystokinin-B receptors (CCK-BR) that are overexpressed in this malignancy. [Leu15]-Gastrin I (human) is promising for research of gastric cancer .
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- HY-P1537
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Neuropeptide Y Receptor
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Metabolic Disease
Endocrinology
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Pancreatic Polypeptide, bovine, a 36-amino acid, straight chain polypeptide derived primarily from the pancreas, inhibits secretin- and cholecystokinin-stimulated pancreatic secretion; Pancreatic Polypeptide, bovine acts as an agonist of NPY receptor, with high affinity at NPYR4.
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- HY-A0261
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ICI-50123
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Cholecystokinin Receptor
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Endocrinology
Cancer
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Pentagastrin (ICI-50123) is a potent, selective Cholecystokinin B (CCKB) receptor antagonists with IC50 values of 11 nM and 1100 nM for CCKB and CCKA, respectively. Pentagastrin enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury . .
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- HY-P2025
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Peptides
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Neurological Disease
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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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- HY-P2055
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Peptides
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Endocrinology
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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 .
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Optimized version of product available:
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Cat. No. |
Product Name |
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Classification |
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- HY-160045
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Aptamers
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AP1153 aptamer sodium is a DNA aptamer that specifically binds to the cholecystokinin receptor CCKBR (Kd: ~15 pM), but does not activate CCKBR-related signaling pathways. AP1153 aptamer sodium is internalized by pancreatic ductal adenocarcinoma (PDAC) cells in a receptor-mediated manner. AP1153 aptamer sodium can bioconjugate to the surface of fluorescent nanoparticles to facilitate nanoparticle delivery to PDAC tumors in vivo .
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