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Etamicastat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Etamicastat图片
CAS NO:760173-05-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
BIA 5-453
产品介绍
Etamicastat (BIA 5-453) 是一种有效且可逆的多巴胺 β-羟化酶 (DBH) 抑制剂,IC50值为 107 nM。可用于心血管疾病的研究。
生物活性

Etamicastat (BIA 5-453) is a potent and reversibledopamine-β-hydroxylase(DBH) inhibitor with anIC50value of 107 nM[1]. Etamicastat can be used in the research of cardiovascular diseases[2].

IC50& Target

IC50: 107 nM (DBH)[1]

体外研究
(In Vitro)

Etamicastat blocks the hERG current amplitude with an IC50value of 44 μg/mL (141 μM)[2].

体内研究
(In Vivo)

Etamicastat (100 mg/kg; administered intraperitoneally) leads to a significant reduction of noradrenaline levels in heart with concomitant increasing in dopamine levels[1].
Etamicastat (50 mg/kg; a single oral administration) exhibits moderate oral bioavailability (64%), Cmax(4.9 nM), and terminal elimination half-lives (T1/2=3.7 h) in male Wistar rats[1].

Animal Model:NMRi mice[1]
Dosage:100 mg/kg
Administration:Administered intraperitoneally
Result:Led to a significant reduction of noradrenaline levels (36% control) in heart with concomitant increasing in dopamine levels (850% of control).
Animal Model:Male Wistar rats[1]
Dosage:50 mg/kg (Pharmacokinetic Analysis)
Administration:Orally administered with at a dose volume of 10 mL/kg
Result:Oral bioavailability (64%), Cmax(4.9 nM), and (T1/2=3.7 h).
Clinical Trial
分子量

311.35

Formula

C14H15F2N3OS

CAS 号

760173-05-5

中文名称

依他米司特

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.