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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 .
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.
KSG-504 (anhydrous) is a CCKreceptor antagonist. KSG-504 (anhydrous) inhibits the development of Ethionine-induced acute pancreatitis in rats and facilitates the regeneration of acinar cells .
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 CCKreceptor. 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 .
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 .
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 .
RP 72540 is a selective CCK-Breceptor antagonist, with IC50 values of 2.4, 1.2, and 3.8 nM for CCK-Breceptors 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 .
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 .
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 .
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 .
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.
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) .
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 .
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) .
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 .
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 .
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 .
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 .
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 .
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 CCKreceptors .
Benzotript (Benzotriptum) is a cholecystokinin-receptor(CCK) and gastrin receptor antagonist. Benzotript shows antiproliferative effects in human colon carcinoma cell lines .
LY 225910 is a selective antagonist for cholecystokinin receptor(CCK2receptor), which affects the excitatory response to morphine, and leads to morphine sensitization .
Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2receptor 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 .
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 CCKreceptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
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 .
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 Ki values of 0.068, 0.62 and 0.19 nM, respectively .
Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [ 3H]CCK-8 to the human CCK-2 receptor with a Ki 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 .
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 CCKreceptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance .
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 CCKreceptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
[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 .
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 .
Enterostatin (rat), an orally active activation peptide of procolipase, selectively reduces fat intake. Enterostatin (rat) reduces serum cholesterol levels by way of a CCK1 receptor-dependent mechanism .
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 .
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 .
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 .
[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 .
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 .
Enterostatin (rat), an orally active activation peptide of procolipase, selectively reduces fat intake. Enterostatin (rat) reduces serum cholesterol levels by way of a CCK1 receptor-dependent mechanism .
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 .
RIPK2 is a multifunctional serine/threonine/tyrosine protein kinase that coordinates innate and adaptive immune responses. It is activated by bacterial peptidoglycan to form filaments in the NOD1 and NOD2 pathways, undergoing autophosphorylation and polyubiquitination. RIPK2 Protein, Human (P. pastoris, His) is the recombinant human-derived RIPK2 protein, expressed by P. pastoris , with C-6*His, C-6*His labeled tag.
DBI, a versatile protein, binds medium- and long-chain acyl-CoA esters, indicating a potential intracellular carrier role. It also displaces diazepam from the benzodiazepine recognition site on the GABA type A receptor. This dual functionality suggests DBI may act as a neuropeptide, modulating GABA receptor activity. Remarkably, DBI functions as a monomer in these interactions. DBI Protein, Human (103a.a, His) is the recombinant human-derived DBI protein, expressed by E. coli , with N-6*His labeled tag.
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