CAS NO: | 760173-05-5 |
包装 | 价格(元) |
250mg | 电议 |
500mg | 电议 |
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 SMILES | S=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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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. |