Nepicastat (SYN-117) HCl
(Synonyms: 盐酸内匹司他,SYN-117 hydrochloride; RS-25560-197 hydrochloride) 目录号 : GC12596An inhibitor of dopamine β-hydroxylase
Cas No.:170151-24-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.50%
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- Datasheet
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.
Cas No. | 170151-24-3 | SDF | |
别名 | 盐酸内匹司他,SYN-117 hydrochloride; RS-25560-197 hydrochloride | ||
化学名 | 4-(aminomethyl)-3-[(2S)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]-1H-imidazole-2-thione;hydrochloride | ||
Canonical SMILES | C1CC2=C(C=C(C=C2CC1N3C(=CNC3=S)CN)F)F.Cl | ||
分子式 | C14H15F2N3S.HCl | 分子量 | 331.81 |
溶解度 | ≥ 16.6 mg/mL in DMSO | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.0138 mL | 15.0689 mL | 30.1377 mL |
5 mM | 0.6028 mL | 3.0138 mL | 6.0275 mL |
10 mM | 0.3014 mL | 1.5069 mL | 3.0138 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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