Etamicastat (BIA 5-453)
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。
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包装价格促销价数量
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250mg￥0.000.00- +
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500mg￥0.000.00- +
- 货号: ajcx12828
- CAS: 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
- 分子式: C14H15F2N3OS
- 分子量: 311.35
- 纯度: ＞98%
- 溶解度: Soluble in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
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.
