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CAS No.: 170151-24-3

Nepicastat HCl Catalog No. CSN13452

Synonyms: SYN-117 hydrochloride;RS-25560-197 hydrochloride;SYN-117 HCl

Nepicastat HCl is a potent and selective dopamine β-hydroxylase (DBH) inhibitor with IC50 value of 9 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Dopamine beta-hydroxylase is an enzyme that catalyzes the conversion of dopamine to norepinephrine. Nepicastat hydrochloride is a dopamine β-hydroxylase inhibitor with IC50 of 8.5 ± 0.8 and 9.0 ± 0.8 nM for bovine and human, respectively^[3]. In vitro, Nepicastat hydrochloride exhibited selective and concentration-dependent inhibition to dopamine-β-hydroxylase in cattle and humans, with IC50 value of 8.5 nM and 9.0 nM, respectively. Nepicastat hydrochloride has quite low affinity for 12 other enzymes and 13 neurotransmitter receptors. In vivo, in the arteries, the left ventricle, and the cerebral cortex of rats with spontaneous hypertension (SHRs), Nepicastat dosage dependently decreased the level of norepinephrine, and increased the dopamine content and dopamine/norepinephrine ratio^[3]. In rat brains, 50 mg/kg (i.p.) dose of Nepicastat hydrochloride led to reduction in the noradrenalin (NE), and block of the recovery of cocaine induced drug addiction ^[4]. In dogs with chronic heart failure, low doses of nepicastat (0.5 mg/kg) are quite suitable to prevent dysfunction and remodeling of the left ventricle (LV), and the combination of nepicastat hydrochloride and enalapril is quite suitable to use in addition to all morphological characteristics^[5]. Nepicastat hydrochloride (3 mg/kg, i.v.), to be quite suitable for the use in SHRs anesthesia, plays the role of antihypertensive; it significantly reduces renal vascular resistance (38%) and increases renal blood flow (22%)^[6].
动物研究
剂量
Rat: 50 mg/kg^[3] (i.p.); 3 mg/kg - 100 mg/kg^[4] (p.o.) Dog: 0.05 mg/kg - 5 mg/kg^[4] (p.o., BID)

给药途径
i.p., p.o.
参考文献

动物研究
剂量	Rat: 50 mg/kg^[3] (i.p.); 3 mg/kg - 100 mg/kg^[4] (p.o.) Dog: 0.05 mg/kg - 5 mg/kg^[4] (p.o., BID)
给药途径	i.p., p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0138 mL
- 15.0688 mL
- 30.1376 mL
- 5 mM
- 0.6028 mL
- 3.0138 mL
- 6.0275 mL
- 10 mM
- 0.3014 mL
- 1.5069 mL
- 3.0138 mL

技术信息

CAS号

170151-24-3

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H16ClF2N3S

运输

蓝冰

分子量

331.81

别名

SYN-117 hydrochloride;RS-25560-197 hydrochloride;SYN-117 HCl;RS 25560197 HCl;Nepicastat (hydrochloride);RS 25560-197;SYN-117;Nepicastat;Nepicastat HCl

溶解度

DMSO	66.0 mg/mL (198.9 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

1% CMC Na+water

20 mg/mL

suspension

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