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Etamicastat(BIA 5-453)
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(BIA 5-453)图片
CAS NO:760173-05-5
包装与价格：
包装价格(元)
250mg电议
500mg电议

产品介绍
Etamicastat (BIA 5-453) (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。
Cas No.760173-05-5
别名(R)-5-(2-氨基乙基)-1-(6,8-二氟苯并二氢吡喃-3-基)-1,3-二氢咪唑-2-硫酮,BIA 5-453
Canonical SMILESS=C1NC=C(CCN)N1[C@H]2COC3=C(C=C(F)C=C3F)C2
分子式C14H15F2N3OS
分子量311.35
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Etamicastat (BIA 5-453) is a potent and reversible peripheral dopamine-β-hydroxylase (DβH) inhibitor[1].

Upon intraperitoneal administration to NMRi mice, Etamicastat (100 mg/ kg) leads to a significant reduction of noradrenaline levels (36% control) in heart with concomitant increasing in dopamine levels (850% of control)[2].Etamicastat (50 mg/kg) is rapidly absorbed into the systemic circulation reaching a maximum concentration at 4 h post-administration, representing 29% of total Etamicastat and quantified metabolites, using AUC0-t as a measure of systemic exposure[2].

[1]. Vaz-da-Silva M, et al. Effect of food on the pharmacokinetic profile of Etamicastat (BIA 5-453). Drugs R D. 2011;11(2):127-36. [2]. Loureiro AI, et al. Etamicastat, a new dopamine-?-hydroxylase inhibitor, pharmacodynamics and metabolism in rat. Eur J Pharmacol. 2014 Oct 5;740:285-94.