Cholecystokinin (CCK) is a neuropeptide that affects growth rate in chickens by regulating appetite. CCK peptides exert their function by binding to two identified receptors, CCKAR and CCKBR in the GI tract and the brain, respectively, as well as in other organs. In mammals, CCK/CCKAR interactions affect a number of immunological parameters, including regulation of lymphocytes and functioning of monocytes.
CCK, also known as pancreozymin, is synthesized and secreted by enteroendocrine cells in the duodenum. The main function of CCK is to cause the release of digestive enzymes and bile from the pancreas and gallbladder, respectively. It also induces drug tolerance to opioids like morphine and heroin. Cholecystokinin (CCK) has strong bioactivity in the regulation of a number of cell activities.
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SR146131 (SR-146131) a small molecule positive allosteric modulator of the type 1 cholecystokinin receptor (CCK1R) with pEC50 of 10.34.
L-365260 (L 365260;L365260) is a potent, selective, orally active cholecystokinin receptor 2 (CCK2) antagonist with IC50 of 2 nM; displays >100-fold selecitvity over CCK1; antagonizes gastrin-stimulated acid secretion in mice (ED50 = 0.03 mg/kg), does not affect basal acid secretion and did not antagonize histamine- or carbachol-stimulated acid secretion.
Netazepide (YF476, Sograzepide) is a potent, selective and orally active gastrin/CCK-2 antagonist with IC50 of 0.1 nM; displays >5,000-fold selectivity over CCK-1 receptors; inhibits pentagastrin-induced gastric acid secretion in anesthetized rats (ED50=87 nM/kg), and shows potential for the treatment of gastroesophageal reflux disease (GERD); also inhibits gastric neuroendocrine enterochromaffin-like (ECL) cell hyperplasia and gastric carcinoid tumor development.
Ceclazepide is a potent, selective cholecystokinin receptor CCK2 antagonist for treatment of gastroesophageal reflux disease (GERD).
JNJ-26070109 (JNJ 26070109;JNJ26070109) is a novel, potent, selective orally active CCK-2 receptor antagonist with pKi of 8.49 for hCCK2; displays >1200-fold selectivity over hCCK1 receptor; has oral EC50 of 1.5 and 0.26 uM in conscious rat and dog chronic gastric fistula models of pentagastrin-stimulated acid secretion, respectively; inhibits gastric acid secretion and prevents omeprazole-induced acid rebound in the rats.
PF-04756956 (PF04756956;PF 04756956) is a potent, selective CCK1 receptor agonist with EC50 of 0.47 nM; elicits no biological response at the CCK2 receptors; demonstrates robust weight loss in a diet-induced obese rat model with very low systemic exposure.
CE-326597 (CE 326597) is a potent, selective agonist of the human and rat CCK1 receptor with Ki of 36 nM; significantly reduces food intake with minimal systemic exposure in rodents.
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