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Ebrotidine

Catalog No. T15195 CAS 100981-43-9

Synonyms: FI3542

Ebrotidine (FI3542) is a competitive H2-receptor antagonist with Ki of 127.5 nM. Ebrotidine has a potent antisecretory activity and evidenced gastroprotection.

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Ebrotidine, CAS 100981-43-9

Pack Size	Availability	Price/USD
2 mg	In stock	$ 37.00
5 mg	In stock	$ 59.00
10 mg	In stock	$ 97.00
1 mL * 10 mM (in DMSO)	In stock	$ 65.00

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Description	Ebrotidine (FI3542) is a competitive H2-receptor antagonist with Ki of 127.5 nM. Ebrotidine has a potent antisecretory activity and evidenced gastroprotection.
Targets&IC50	H2 receptor:127.5 nM(Ki)
In vitro	Ebrotidine displaced 3H-thiotidine specific binding to histamine H2-receptors (Ki: 127.5 nmol/l), showing a higher affinity (p < 0.05) than ranitidine (Ki: 190.0 nmol/l) and cimetidine (Ki: 246.1 nmol/l) [1].
In vivo	Ebrotidine inhibited histamine- and pentagastrin-stimulated acid secretion in a dose-dependent manner (ED50: 0.21 and 0.44 mg/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 1h. 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].

Synonyms	FI3542
Molecular Weight	477.42
Formula	C14H17BrN6O2S3
CAS No.	100981-43-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (209.46 mM), Sonication is recommended.

References and Literature

1. Agut J, Sánchez JC, Sacristán A, Action of ebrotidine, ranitidine and cimetidine on the specific binding to histamine H1- and H2-receptors. Arzneimittelforschung. 1997 Apr;47(4A):447-9. 2. Palop D, Agut J, Márquez M, Histamine H2-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. 3. Piotrowski J, Yamaki K, Morita M, Ebrotidine--a new H2-receptor antagonist with mucosal strengthening activity. Biochem Int. 1992 Mar;26(4):659-67. 4. 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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library GPCR Compound Library Membrane Protein-targeted Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library ReFRAME Related Library Drug-induced Liver Injury (DILI) Compound Library FDA-Approved & Pharmacopeia Drug Library Bioactive Compound Library Human Metabolite Library

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Keywords

Ebrotidine 100981-43-9 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor FI 3542 FI-3542 FI3542 inhibit Inhibitor inhibitor

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