Ebrotidine, Inhibitor

Ebrotidine

Cat. Num. AAA5754814

• Purity: 98.00%
• Synonyms: Ebrotidine; FI3542; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 100mg/mL (209.46mM) Need ultrasonic; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C14H17BrN6O2S3
• SMILES: O=S(C1=CC=C(Br)C=C1)(/N=C/NCCSCC2=CSC(NC(N)=N)=N2)=O
• CAS Number: 100981-43-9
• Target & IC50: Others
• In Vitro: Ebrotidine inhibited histamine- and pentagastrin-stimulated acid secretion in a dose-dependent manner (ED50: 0.21 and 0.44mg/kg, respectively), following intravenous administration to rats [2]. Results of the macroscopic assessment revealed that ebrotidine at doses of 50mg and higher/kg body weight effectively prevented mucosal injury and that the maximal protective effect was achieved by 1hours. Physicochemical analysis established that ebrotidine evoked 30% increase in mucus gel dimension, and showed a 20% increase in phospholipids, and the content of sulfo- (18%) and sialomucins (21%) [4]. The mean number of gastric erosions seen at endoscopy after treatment with ebrotidine plus ASA (2.0 +/- 0.3) was obviously lower than that after placebo plus ASA (3.7 +/- 0.2). This reduction in lesion core by ebrotidine was accompanied by a significant increase in gastric blood flow (by 15% in corpus and 26% in antrum), by a rise in transmucosal potential difference (by 12%), and by a decrease of mucosal micro bleeding [3].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Ebrotidine, inhibitor

Ebrotidine is a competitive H2-receptor antagonist (Ki: 127.5nM). It has a potent antisecretory activity and evidenced gastroprotection.

References

Agut J, Sanchez JC, Sacristan A, Action of ebrotidine, ranitidine and cimetidine on the specific binding to histamine H- and H2-receptors. Arzneimittelforschung. 1997 Apr;47(4A):447-9.
Agut J, Sanchez JC, Sacristan A, Action of ebrotidine, ranitidine and cimetidine on the specific binding to histamine H- and H2-receptors. Arzneimittelforschung. 1997 Apr;47(4A):447-9.
Palop D, Agut J, Marquez M, histamine H-receptor antagonist action of ebrotidine. Effects on gastric acid secretion, gastrin levels and NSAID-induced gastrotoxicity in the rat. Arzneimittelforschung. 1997 Apr;47(4A):439-46.
Palop D, Agut J, Marquez M, histamine H-receptor antagonist action of ebrotidine. Effects on gastric acid secretion, gastrin levels and NSAID-induced gastrotoxicity in the rat. Arzneimittelforschung. 1997 Apr;47(4A):439-46.
Konturek SJ, Kwiecien N, Sito E, Effects of ebrotidine on aspirin-induced gastric mucosal damage and blood flow in humans. Scand J Gastroenterol. 1993 Dec;28(12):1047-50.
Konturek SJ, Kwiecien N, Sito E, Effects of ebrotidine on aspirin-induced gastric mucosal damage and blood flow in humans. Scand J Gastroenterol. 1993 Dec;28(12):1047-50.
Piotrowski J, Yamaki K, Morita M, Ebrotidine--a new H2-receptor antagonist with mucosal strengthening activity. Biochem Int. 1992 Mar;26(4):659-67.
Piotrowski J, Yamaki K, Morita M, Ebrotidine--a new H2-receptor antagonist with mucosal strengthening activity. Biochem Int. 1992 Mar;26(4):659-67.