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Nepicastat hydrochloride

Nepicastat hydrochloride (RS-25560-197 hydrochloride) 是一种选择性的，有效的，口服活性的多巴胺 β 羟化酶(dopamine-beta-hydroxylase)抑制剂，对牛和人多巴胺 β 羟化酶的IC50分别为IC50=8.5 nM 和IC50=9 nM。Nepicastat HCl 可以穿过血脑屏障。

CAS号

170151-24-3

分子式

C14H15F2N3S·HCl

主要靶点

Hydroxylase

仅限科研使用

Cat No : CM04676

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Synonyms

Nepicastat HCl|SYN-117 hydrochloride|RS-25560-197 hydrochloride|内匹司他盐酸盐|Nepicastat (SYN-117) HCl

验证数据展示

  • CAS No.: 170151-24-3

    Nepicastat hydrochloride
    CAS#: 170151-24-3

产品信息

Nepicastat hydrochloride (RS-25560-197 hydrochloride) 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.

CAS号 170151-24-3
分子式 C14H15F2N3S·HCl
主要靶点 Hydroxylase
主要通路 代谢
分子量 331.81
纯度 98.35%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 Nepicastat HCl|SYN-117 hydrochloride|RS-25560-197 hydrochloride|内匹司他盐酸盐|Nepicastat (SYN-117) HCl

靶点活性

Bovine dopamine-beta-hydroxylase:8.5 nM|HμMan dopamine-beta-hydroxylase:9 nM

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]

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]

溶解度

DMSO:33.2 mg/mL (100 mM)

参考文献

1.Stanley WC, et al. Br J Pharmacol. 1997, 121(8), 1803-1809.
2.Stanley WC, et al. J Cardiovasc Pharmacol. 1998, 31(6), 963-970.
3.Sabbah HN, et al. Circulation. 2000, 102(16), 1990-1995.
4.Schroeder JP, et al. Neuropsychopharmacology. 2010, 35(12), 2440-2449.

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