更新時(shí)間:2024-11-17
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(R)-Nepicastat HCl 195881-94-8
(R)-Nepicastat HCl
分子式:C14H15F2N3S.HCl 分子量:331.81
產(chǎn)品描述
(R)-Nepicastat HCl是Nepicastat HCl的R-對(duì)映體,是有效的,選擇性抑制劑,作用于牛和人類dopamine-β-hydroxylase(多巴胺-β-羥化酶),IC50分別為25.1 nM和 18.3 nM,對(duì)12種其他酶和13種神經(jīng)遞質(zhì)受體具有極其微弱的親和力。
靶點(diǎn)
Bovine dopamine-beta-hydroxylase
Human dopamine-β-hydroxylase
IC50
25.1 nM
18.3 nM
體外研究
(R)-Nepicastat produces concentration-dependent inhibition of bovine and human dopamine-β-hydroxylase activity in vitro.
體內(nèi)研究
(R)-Nepicastat (30 mg/kg, p.o.) reduces noradrenaline content, dopamine content and dopamine/noradrenaline ratio in mesenteric artery and left ventricle of spontaneously hypertensive rats (SHRs).
溶解性
DMSO 66 mg/mL,水 <1 mg/mL,乙醇 <1 mg/mL
穩(wěn)定性
2年 -20°C粉狀,6月-80°C溶于DMSO