862583-15-1

862583-15-1 structure

Name: Gastrazole
Chemical Name: disodium,5-[[(2S)-2-[[6-(cycloheptylmethylcarbamoyl)-1H-benzimidazole-5-carbonyl]amino]-3-(2-fluorophenyl)propanoyl]amino]benzene-1,3-dicarboxylate
CAS Number: 862583-15-1
Molecular Formula: C₃₄H₃₂FN₅Na₂O₇
Molecular Weight: 687.62500
Catalog: Signaling Pathways GPCR/G Protein Cholecystokinin Receptor
Create Date: 2017-05-18 05:03:14
Modify Date: 2024-01-09 18:11:28
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[1][2].

Name	disodium,5-[[(2S)-2-[[6-(cycloheptylmethylcarbamoyl)-1H-benzimidazole-5-carbonyl]amino]-3-(2-fluorophenyl)propanoyl]amino]benzene-1,3-dicarboxylate
Synonyms	unii-55tzm8f95p

Description	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[1][2].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> GPCR/G Protein >> Cholecystokinin Receptor
Target	CCK2/gastrin receptor[1]
In Vivo	Gastrazole (0.15-3 μmol/kg; i.v.) dose-dependently inhibits the Pentagastrin-stimulated gastric acid secretion[2]. Animal Model: Male Sprague-Dawley rats with a gastric fistula[2] Dosage: 0.15, 0.3, 3 mg/kg Administration: Intravenous administration Result: Dose-dependently inhibited Pentagastrin-stimulation acid secretion by maximally 73%.
References	[1]. Chau I, et, al. Gastrazole (JB95008), a novel CCK2/gastrin receptor antagonist, in the treatment of advanced pancreatic cancer: results from two randomised controlled trials. Br J Cancer. 2006 Apr 24;94(8):1107-15. [2]. Rudholm T, et, al. Release of regulatory gut peptides somatostatin, neurotensin and vasoactive intestinal peptide by acid and hyperosmolal solutions in the intestine in conscious rats. Regul Pept. 2009 Jan 8;152(1-3):8-12.