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Cat. No. Product Name CAS No. Information
PC-60082

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.

Gastric Cancer

Phase 2 Clinical

PC-70239

L-365260

118101-09-0 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.

Anxiety

Discontinued

PC-70198

PF-04756956

1228934-52-8 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.
PC-70197

CE-326597

870615-40-0 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.

Obesity

Phase 2 Discontinued

PC-70196

JNJ-26070109

844645-08-5 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.
PC-60036

Ceclazepide

1801749-44-9 A potent, selective cholecystokinin receptor CCK2 antagonist for treatment of gastroesophageal reflux disease (GERD).

Other Indication

Phase 1 Clinical

PC-45389

Z-360

209219-38-5 A novel potent, orally active CCK-2/gastrin receptor antagonist with Ki of 0.47 nM; significantly reduces gastrin-induced PKB/Akt phosphorylation in human CCK-2 receptor-expressing cells; significantly inhibits the growth of MiaPaCa2, also suppresses pancreatic tumor growth and prolong survival in a pancreatic carcinoma xenograft model combined with gemcitabine; prevents up-regulation of ephrin B1 gene expression and phosphorylation of NR2B via suppression of interleukin-1 β production in a cancer-induced pain model in mice.

Pancreatic Cancer

Phase 2 Clinical

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