首页 Metabolism Hydroxylase Nepicastat HCl
Nepicastat HCl
编号 T6604     别名: RS-25560-197 hydrochloride, Nepicastat hydrochloride, SYN-117 hydrochloride, Nepicastat (SYN-117) HCl, SYN-117 hydrochloride, Nepicastat (SYN-117) HCl, RS-25560-197 hydrochloride Nepicastat hydrochloride
CAS 170151-24-3     分子式 C14H15F2N3S·HCl     分子量 331.81
靶点: Dopamine β-hydroxylase;
Nepicastat (SYN-117) HCl is an effective and specific inhibitor, which is used for bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, respectively.The affinity of Nepicastat for twelve other enzymes and thirteen neurotransmitter receptors is negligible.
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规格 库存 单价 数量
5 mg 上海现货 573.00
10 mg 上海现货 933.00
50 mg 上海现货 2733.00
100 mg 上海现货 4919.00
1 mL * 10 mM (in DMSO) 上海现货 573.00
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生物活性

产品描述

Nepicastat (SYN-117) HCl is an effective and specific inhibitor, which is used for bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, respectively.The affinity of Nepicastat for twelve other enzymes and thirteen neurotransmitter receptors is negligible.

靶点活性

Dopamine β-hydroxylase,9nM

体外活性

In vitro, Nepicastat hydrochloride shows the selective and concentration-dependent inhibition effects on bovine and human dopamine-beta-hydroxylase activity with IC50 of 8.5 nM and 9.0 nM, respectively. While Nepicastat hydrochloride has negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. [1]

体内活性

In the artery, left ventricle and cerebral cortex of spontaneously hypertensive rats (SHRs), Nepicastat hydrochloride reduces noradrenaline content, and increases dopamine content and dopamine/noradrenaline ratio in a dose-dependent manner. In addition, Nepicastat hydrochloride also produces the similar effects on noradrenaline, dopamine and dopamine/noradrenaline ratio in tissues and plasma of beagle dogs. [1] In inactin-anesthetized SHRs, Nepicastat hydrochloride (3 mg/kg, i.v.) produces the antihypertensive effects and causes a significant decrease in renal vascular resistance (38%) and an increase in renal blood flow (22%). [2] In dogs with chronic heart failure, low-dose Nepicastat hydrochloride (0.5 mg/kg) prevents left ventricular (LV) dysfunction and remodeling, and combination therapy of Nepicastat hydrochloride and enalapril results in additional improvements in all morphological features. [3] In rat brain, Nepicastat hydrochloride at a dose of 50 mg/kg ( i.p.) leads to the reduction of norepinephrine (NE) and blocks cocaine-primed reinstatement of cocaine seeking. [4]

动物实验

动物模型:Spontaneously hypertensive rats (SHRs).

化学信息

分子量

331.81

分子式

C14H15F2N3S·HCl

CAS

170151-24-3

溶解度

DMSO: 33.2 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 3.014 ml 15.069 ml 30.138 ml
5 mM 0.603 ml 3.014 ml 6.028 ml
10 mM 0.301 ml 1.507 ml 3.014 ml
50 mM 0.06 ml 0.301 ml 0.603 ml
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