Etamicastat hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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

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

Etamicastat (100 mg/kg; administered intraperitoneally) leads to a significant reduction of noradrenaline levels in heart with concomitant increasing in dopamine levels.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.Animal Model:NMRi mice Dosage:100 mg/kg Administration:Administered intraperitoneallyResult: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 ratsDosage:50 mg/kg (Pharmacokinetic Analysis) Administration:Orally administered with at a dose volume of 10 mL/kg Result:Oral bioavailability (64%), Cmax (4.9 nM), and (T1/2=3.7 h).

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Metabolic Enzyme/Protease

Dehydrogenase

Dehydrogenase

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677773-32-9

347.81

C14H16ClF2N3OS

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (287.51 mM; 超声助溶 ) H2O 中的溶解度 : 16.67 mg/mL (47.93 mM; 超声助溶)

Cl.NCCc1c[nH]c(=S)n1[C@H]1COc2c(F)cc(F)cc2C1

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(-20℃)

With Ice Pack

≥ 2 years