Etamicastat

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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。

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%), C_max(4.9 nM), and terminal elimination half-lives (T_1/2=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%), C_max(4.9 nM), and (T_1/2=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.