Ebrotidine

CAT: 0804-HY-15538-01Size: 5 mgDry Ice: NoHazardous: No

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CAT#:0804-HY-15538-01Size:5 mg

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Description

Ebrotidine (FI 3542) is a competitive H2-receptor antagonist (Ki= 127.5 nM) with a potent antisecretory activity and evidenced gastroprotection. IC50 Value: 127.5 nM (Ki) [1]; 0.21mg/kg (ED50, histamine- stimulated acid secretion) [2] Target: H2 receptor 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: Following intravenous administration to rats, ebrotidine inhibited histamine- and pentagastrin-stimulated acid secretion in a dose-dependent manner, ED50 being 0.21 and 0.44 mg/kg, respectively [2]. The mean number of gastric erosions seen at endoscopy after treatment with ebrotidine plus ASA (2.0 +/- 0.3) was significantly 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 microbleeding [3]. Results of 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 20% increase in phospholipids, and the content of sulfo- (18%) and sialomucins (21%) [4].

CAS Number

100981-43-9

Product Name Alternative

FI3542

UNSPSC

12352005

Target

Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Endocrinology

Assay Protocol

https://www.medchemexpress.com/Ebrotidine.html

Concentration

10mM

Purity

98.51

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=S(C1=CC=C(Br)C=C1)(/N=C/NCCSCC2=CSC(NC(N)=N)=N2)=O

Molecular Formula

C14H17BrN6O2S3

Molecular Weight

477.42

References & Citations

[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]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.|[4]Piotrowski J, Yamaki K, Morita M, Ebrotidine--a new H2-receptor antagonist with mucosal strengthening activity. Biochem Int. 1992 Mar;26 (4) :659-67.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

H2 Receptor

Alternative Products

Catalog	Name
TRC-E320550-50MG	Ebrotidine
A15075-100	Ebrotidine 100mg
A15075-50	Ebrotidine 50mg
A15075-10	Ebrotidine 10mg
A15075-5	Ebrotidine 5mg
A15075-2	Ebrotidine 2mg
A15075-10mM-D	Ebrotidine 10mM * 1mL in DMSO

Ebrotidine

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