产品名称

英文名称：Ebrotidine

同义词

Ebrotidine、100981-43-9、FI-3542、Ebrotidine [INN]、TMZ3IBW2OW、N-(4-bromophenyl)sulfonyl-N'-[2-[[2-(diaminomethylideneamino)-1,3-thiazol-4-yl]methylsulfanyl]ethyl]methanimidamide、Ebrotiding、Ebrotidinum [Latin]、Ebrotidina [Spanish]、Ebrotidina、Ebrotidinum、Ebroc

产品性质

CAS编号：100981-43-9

分子式：C14H17BrN6O2S3

分子量：477.42

PubChem编号：65869

英文别名：Ebrotidine|100981-43-9|FI-3542|Ebrotidine [INN]|TMZ3IBW2OW|N-(4-bromophenyl)sulfonyl-N'-[2-[[2-(diaminomethylideneamino)-1,3-thiazol-4-yl]methylsulfanyl]ethyl]methanimidamide|Ebrotiding|Ebrotidinum [Latin]|Ebrotidina [Spanish]|Ebrotidina|Ebrotidinum|Ebroc

规格或纯度：≥98%

英文名称：Ebrotidine

生化机理：DescriptionIC50 Value 127.5nM(Ki)[1]; 0.21mg/kg (ED50, histamine- stimulated acid secretion) [2]Ebrotidine is a competitive H2-receptor antagonist with a potent antisecretory activity and evidenced gastroprotection.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].Clinical trial N/A

储存温度：-20°C储存

运输条件：超低温冰袋运输

ALogP：1.5

IUPAC Name：N-(4-bromophenyl)sulfonyl-N'-[2-[[2-(diaminomethylideneamino)-1,3-thiazol-4-yl]methylsulfanyl]ethyl]methanimidamide

INCHI：InChI=1S/C14H17BrN6O2S3/c15-10-1-3-12(4-2-10)26(22,23)19-9-18-5-6-24-7-11-8-25-14(20-11)21-13(16)17/h1-4,8-9H,5-7H2,(H,18,19)(H4,16,17,20,21)

InChi Key：ZQHFZHPUZXNPMF-UHFFFAOYSA-N

Canonical SMILES：C1=CC(=CC=C1S(=O)(=O)NC=NCCSCC2=CSC(=N2)N=C(N)N)Br

Isomeric SMILES：C1=CC(=CC=C1S(=O)(=O)NC=NCCSCC2=CSC(=N2)N=C(N)N)Br

PubChem CID：65869

溶解性：25°C DMSO

产品包装