(R)-NepicaSTAT HCl 是 NepicaSTAT HCl 的 R-对映异构体,是一种有效的选择性抑制剂,对牛和人多巴胺-β-羟化酶的 IC50 分别为 25.1 nM 和 18.3 nM,对其他 12 种酶和 13 种神经递质受体的亲和力可忽略不计.
产品描述
(R)-Nepicastat HCl, the R-enantiomer of Nepicastat HCl, is a potent and selective inhibitor with IC50 of 25.1 nM and 18.3 nM for bovine and human dopamine-β-hydroxylase, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors.
体外活性
(R)-Nepicastat produces concentration-dependent inhibition of bovine and human dopamine-β-hydroxylase activity in vitro. [1]
体内活性
(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). [1]
Cas No.
195881-94-8
分子式
C14H16ClF2N3S
分子量
331.81
别名
RS-25560-198 HCl;盐酸内匹司他
储存和溶解度
H2O:<1 mgml
Ethanol:<1 mgml
DMSO:61 mg/mL (183.8 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years