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Etamicastat hydrochloride
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 hydrochloride图片
规格:98%
分子量:347.81
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Etamicastat hydrochloride (BIA 5-453 hydrochloride) 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。
货号:ajcx29322
CAS:677773-32-9
分子式:C14H16ClF2N3OS
分子量:347.81
溶解度:DMSO: 100 mg/mL (287.51 mM)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC50 value of 107 nM[1]. Etamicastat can be used in the research of cardiovascular diseases[2].

Etamicastat blocks the hERG current amplitude with an IC50 value of 44 μg/mL (141 μM)[2].

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]

[1]. Loureiro AI, et al. Etamicastat, a new dopamine-ß-hydroxylase inhibitor, pharmacodynamics and metabolism in rat. Eur J Pharmacol. 2014 Oct 5;740:285-94. [2]. ManuelVaz-da-Silva, et al. Cardiac safety profile of etamicastat, a novel peripheral selective dopamine-β-hydroxylase inhibitor in non-human primates, human young and elderly healthy volunteers and hypertensive patients. IJC Metabolic & Endocrine. 2015 Jun; (7): 10-24