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Nepicastat (SYN-117) HCl

现货
Catalog No.
A4332
多巴胺-β-羟化酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 770.00
现货
5mg
¥ 700.00
现货
10mg
¥ 1,200.00
现货
50mg
¥ 5,400.00
现货

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Background

Nepicastat (SYN-117) HCl is a potent and selective inhibitor of dopamine-β-hydroxylase with IC50 values of 8.5 and 9.0 nM in bovine and human, respectively [1].

Dopamine-β-hydroxylase is an enzyme involved in the synthesis of small-molecule membrane-bound neurotransmitters. Dopamine-β-hydroxylase catalyses the synthesis of noradrenaline [1].

Nepicastat (SYN-117) HCl is a potent and selective dopamine-β-hydroxylase inhibitor. (R)-Nepicastat exhibited 2-3 fold less potent than nepicastat [1].

In beagle dogs and spontaneously hypertensive rats, nepicastat reduced noradrenaline in a dose-dependent way and increased dopamine and dopamine/noradrenaline ratio in cerebral cortex, left ventricle and the artery. In beagle dogs, nepicastat (2 mg/kg) significantly reduced noradrenaline by 52% and increased dopamine by 646% and dopamine/noradrenaline ratio in plasma [1]. In pithed spontaneously hypertensive rats, nepicastat inhibited the pressor and positive chronotropic due to preganglionic sympathetic nerve stimulation. In spontaneously hypertensive rats, nepicastat (3 mg/kg) exhibited antihypertensive effects and reduced renal vascular resistance by 38% [2]. In rats, nepicastat significantly increased extracellular dopamine accumulation induced by cocaine and amphetamine in the medial prefrontal cortex [3].

References:
[1].  Stanley WC, Li B, Bonhaus DW, et al. Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase. Br J Pharmacol, 1997, 121(8): 1803-1809.
[2].  Stanley WC, Lee K, Johnson LG, et al. Cardiovascular effects of nepicastat (RS-25560-197), a novel dopamine beta-hydroxylase inhibitor. J Cardiovasc Pharmacol, 1998, 31(6): 963-970.
[3].  Devoto P, Flore G, Saba P, et al. The dopamine beta-hydroxylase inhibitor nepicastat increases dopamine release and potentiates psychostimulant-induced dopamine release in the prefrontal cortex. Addict Biol, 2014, 19(4): 612-622.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt331.81
Cas No.170151-24-3
FormulaC14H15F2N3S.HCl
Solubility≥16.6 mg/mL in DMSO, <2.58 mg/mL in EtOH, <2.27 mg/mL in H2O
Chemical Name4-(aminomethyl)-3-[(2S)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]-1H-imidazole-2-thione;hydrochloride
SDFDownload SDF
Canonical SMILESC1CC2=C(C=C(C=C2CC1N3C(=CNC3=S)CN)F)F.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

描述 Nepicastat是一种强效的和选择性的牛和人体多巴胺β-羟化酶抑制剂,IC50值分别为8.5 nM和9 nM。
靶点 bovine dopamine-β-hydroxylase human dopamine-β-hydroxylase        
IC50 8.5 nM 9 nM        

质量控制

化学结构

Nepicastat (SYN-117) HCl