产品
编 号：F611690
分子式：C14H16ClF2N3OS
分子量：347.81
分子式：C14H16ClF2N3OS
分子量：347.81
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 677773-32-9
产品详情
生物活性：
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.
体内研究：
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 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
Dosage: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).
体外研究：
Etamicastat blocks the hERG current amplitude with an IC50 value of 44 μg/mL (141 μM).
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.
体内研究：
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 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
Dosage: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).
体外研究：
Etamicastat blocks the hERG current amplitude with an IC50 value of 44 μg/mL (141 μM).
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