Nepicastat hydrochloride|170151-24-3|(SYN-117 hydrochloride; RS-25560-197 hydrochloride)-陌孚医药/Medlife

您当前的位置：

Nepicastat hydrochloride (Synonyms: SYN-117 hydrochloride; RS-25560-197 hydrochloride)

目录号: PL13549 纯度: ≥98%

Nepicastat hydrochloride (SYN-117 hydrochloride) 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 hydrochloride 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 hydrochloride 可越过血脑屏障。

CAS No. :170151-24-3

商品编号	规格	价格	会员价
PL13549-5mg	5mg	¥964.00	请登录
PL13549-10mg	10mg	¥1607.00	请登录
PL13549-50mg	50mg	¥4821.00	请登录
PL13549-100mg	100mg	¥8438.00	请登录
PL13549-200mg	200mg	询价	询价
PL13549-500mg	500mg	询价	询价
PL13549-10mM*1mLinDMSO	10mM*1mLinDMSO	¥1060.00	请登录

Medlife所售产品仅用于科学研究（非临床研究），非药品不可食用，不可用于人体或动物的临床诊断和治疗，我们不为个人提供产品及服务。产品COA等资料，可至下方“质量控制”中下载。

加入购物车在线咨询收藏产品大包装询价

中文名称	Nepicastat hydrochloride
中文别名	(S)-5-(氨基甲基)-1-(5,7-二氟-1,2,3,4-四氢萘-2-基)-1H-咪唑-2(3h)-硫酮盐酸盐;Nepicastat (SYN-117) HCl 抑制剂;内匹司他盐酸盐;盐酸内匹司他;Nepicastat (SYN-117) HCl;NEPICASTAT HYDROCHLORIDE;(S)-5-(氨基甲基)-1-(5,7-二氟-1,2,3,4-四氢萘-2-基)-1H-咪唑-2(3H)-硫酮盐酸盐
英文名称	Nepicastat hydrochloride
英文别名	(S)-5-(Aminomethyl)-1-(5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)-1H-imidazole-2(3H)-thione hydrochloride;2H-Imidazole-2-thione,5-(aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-...;2H-Imidazole-2-thione,5-(aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-,hydrochloride (1:1;2H-Imidazole-2-thione,5-(aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-,hydrochloride (1:1);Nepicastat (SYN-117) HCl;Nepicastat Hydrochloride;CHEMBL536282;Nepitat (SYN-117) HCl;Nepitat HCl;Nepitat hydrochloride;RS-25560-197;RS-25560-197 hydrochloride;SYN117;SYN-117 hydrochloride;UNII-3WK068D17I;5-(Aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-2H-imidazole-2-thione hydrochloride;SYN-117;RS 25560-197;SYN-117 HCl;Nepicastat (SYN117)HCI;Nepicastat (SYN-117) hydrochloride;Nepicastat HCl (SYN-117),Nepicastat hydrochloride,;RS 25560-197 Nepicastat hydrochloride;(S)-5-(Aminomethyl)-1-(5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)-1H-imidazole-2(3H)-thio;Nepicastat HCl;Nepicastat hydrochloride anhydrous;Nepicastat (hydrochloride);3WK068D17I;(S)-5-(AMINOMETHYL)-1-(5,7-DIFLUORO-1,2,3,4-TETRAHYDRONAPHTHALEN-2-YL)-1H-IMIDAZOLE-2(3H)-THIONE HCL;AK105009;nepicastat-hydrochloride;Nepicastat hydrochloride;Nepicastat(h;Nepicastat HCl, >=99%;RS-25560-197 hydrochloride);Nepicastat Hydrochloride (SYN-117 hydrochloride
Cas No.	170151-24-3
分子式	C₁₄H₁₆ClF₂N₃S
分子量	331.81
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Nepicastat hydrochloride (SYN-117 hydrochloride) 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 hydrochloride 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 hydrochloride 可越过血脑屏障。

生物活性

Nepicastat hydrochloride (SYN-117 hydrochloride) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat hydrochloride produces concentration-dependent inhibition of bovine (IC 50 =8.5 nM) and human (IC 50 =9 nM) dopamine-beta-hydroxylase. Nepicastat hydrochloride can cross the blood-brain barrier (BBB).

性状

Solid

IC50 & Target[1][2]

IC50: 8.5 nM (bovine dopamine-beta-hydroxylase), 9 nM (human dopamine-beta-hydroxylase)

体内研究(In Vivo)

Nepicastat hydrochloride (SYN-117 hydrochloride) (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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Beliaev A, et al. Synthesis and biological evaluation of novel, peripherally selective chromanyl imidazolethione-based inhibitors of dopamine beta-hydroxylase.J Med Chem. 2006 Feb 9;49(3):1191-7.
[2]. Stanley WC, et al. Cardiovascular effects of nepicastat (RS-25560-197), a novel dopamine beta-hydroxylase inhibitor. J Cardiovasc Pharmacol. 1998 Jun;31(6):963-70.

溶解度数据	In Vitro: DMSO : 6 mg/mL (18.08 mM; Need ultrasonic)H₂O : 2 mg/mL (6.03 mM; Need ultrasonic and warming)配制储备液

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

相关产品

The molarity calculator equation

The dilution calculator equation