Racecadotril

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Racecadotril (Acetorphan) 是一种中性内肽酶 (NEP) 抑制剂。Racecadotril 及其活性代谢物 Thiorphan 抑制小鼠脑中纯化的 NEP 活性，Ki 分别为 4500 和 6.1 nM。具有止泻效果。

Racecadotril, also known as acetorphan, is an antidiarrheal drug which acts as a peripherally acting enkephalinase inhibitor.(In Vivo):In mice, following i.v. administration, Racecadotril is rapidly metabolized to Thiorphan; thus, 30?min after the injection only Thiorphan is recovered from the kidney whereas the parent compound Racecadotril is not detected.In rats 92% of a single-dose (10?mg/kg) of radioactively labeled Racecadotril is eliminated within 24?h.Racecadotril is a neutral endopeptidase (NEP) inhibitor with known antidiarrheal activity in animals. Orally administered Racecadotril (100 mg/kg ) shows efficacy in a rat model of castor oil-induced diarrhea.

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In mice, following i.v. administration, Racecadotril is rapidly metabolized to Thiorphan; thus, 30?min after the injection only Thiorphan is recovered from the kidney whereas the parent compound Racecadotril is not detected. In rats 92% of a single-dose (10?mg/kg) of radioactively labeled Racecadotril is eliminated within 24?h.Racecadotril is a neutral endopeptidase (NEP) inhibitor with known antidiarrheal activity in animals. Orally administered Racecadotril (100 mg/kg ) shows efficacy in a rat model of castor oil-induced diarrhea. Animal Model:6-to-7-week-old male Wistar rats Dosage:100 mg/kg Administration:A single oral treatment; 30 minutes before castor oil administration.Result:Significantly reduced stool output but did not prevent the occurrence of diarrhea (100% incidence).

Acetorphan

Proteasome/Ubiquitin

Proteasome

Endopeptidase

Neurological Disease

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81110-73-8

385.49

C21H23NO4S

>98% (HPLC)

DMSO: 22mg/ml(57.07 mM);Water: <1mg/ml;Ethanol: 77mg/ml(199.75 mM)

CC(=O)SCC(CC1=CC=CC=C1)C(=O)NCC(=O)OCC1=CC=CC=C1

benzyl (3-(acetylthio)-2-benzylpropanoyl)glycinate

(-20℃)

With Ice Pack

≥ 2 years