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You are here:Home-Inhibitors & Agonists-GPCR-Cholecystokinin Receptor

Request The Product List ofCholecystokinin Receptor Cholecystokinin Receptor

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.

Cat. No. Product Name CAS No. Information
GY10365

SR146131

221671-61-0

SR146131 (SR-146131) a small molecule positive allosteric modulator of the type 1 cholecystokinin receptor (CCK1R) with pEC50 of 10.34.

GY06191

L-365260

118101-09-0

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.

GY06159

Netazepide

155488-25-8

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.

GY06147

Ceclazepide

1801749-44-9

Ceclazepide is a potent, selective cholecystokinin receptor CCK2 antagonist for treatment of gastroesophageal reflux disease (GERD).

GY06111

JNJ-26070109

844645-08-5

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.

GY05831

PF-04756956

1228934-52-8

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.

GY05695

CE-326597

870615-40-0

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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