Nepicastat

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Nepicastat

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

173997-05-2

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

SYN117
RS-25560-197

产品介绍

Nepicastat (SYN117) 是一种选择性的，有效的，具有口服活性的多巴胺 β 羟化酶(dopamine-beta-hydroxylase)抑制剂。Nepicastat (SYN117) 对牛 (IC₅₀=8.5 nM) 和人(IC₅₀=9 nM) 多巴胺 β 羟化酶产生浓度依赖性抑制作用。Nepicastat (SYN117) 可越过血脑屏障。

生物活性

Nepicastat (SYN117) is a selective, potent, and orally active inhibitor ofdopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC₅₀=8.5 nM) and human (IC₅₀=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB)^[1]^[2]^[3].

IC₅₀& Target

IC50: 8.5 nM (bovine dopamine-beta-hydroxylase), 9 nM (human dopamine-beta-hydroxylase)^[2]

体内研究
(In Vivo)

Nepicastat (3-100 mg/kg; p.o.; three consecutive times, 12 hours apart times) produces dose-dependent decreases in noradrenaline content, increases in dopamine content and increases in dopamine/noradrenaline ratio in the artery (mesenteric or renal), left ventricle^[3].

Animal Model:	15-16 weeks male spontaneously hypertensive rats (SHRs)^[3]
Dosage:	Oral administration; three consecutive times, 12 hours apart
Administration:	3, 10, 30, 100 mg/kg
Result:	Produced dose-dependent decreases in noradrenaline content, increases in dopamine content and increases in dopamine/noradrenaline ratio in the artery (mesenteric or renal), left ventricle and cerebral cortex.

Clinical Trial

分子量

295.35

Formula

C₁₄H₁₅F₂N₃S

CAS 号

173997-05-2

中文名称

内匹司他

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据

In Vitro:

DMSO : ≥ 48 mg/mL(162.52 mM)

*"≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	3.3858 mL	16.9291 mL	33.8581 mL
5 mM	0.6772 mL	3.3858 mL	6.7716 mL
10 mM	0.3386 mL	1.6929 mL	3.3858 mL