Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Nepicastat hydrochloride (RS-25560-197 hydrochloride) 是一种选择性的,有效的,口服活性的多巴胺 β 羟化酶(dopamine-beta-hydroxylase)抑制剂,对牛和人多巴胺 β 羟化酶的IC50分别为IC50=8.5 nM 和IC50=9 nM。Nepicastat HCl 可以穿过血脑屏障。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 218 | 现货 | ||
5 mg | ¥ 492 | 现货 | ||
10 mg | ¥ 828 | 现货 | ||
25 mg | ¥ 1,490 | 现货 | ||
50 mg | ¥ 2,490 | 现货 | ||
100 mg | ¥ 4,370 | 现货 | ||
500 mg | ¥ 9,160 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 547 | 现货 |
产品描述 | Nepicastat hydrochloride (RS-25560-197 hydrochloride) is an effective and specific inhibitor, which is used for bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, respectively.The affinity of Nepicastat for twelve other enzymes and thirteen neurotransmitter receptors is negligible. |
靶点活性 | HμMan dopamine-beta-hydroxylase:9 nM, Bovine dopamine-beta-hydroxylase:8.5 nM |
体外活性 | In vitro, Nepicastat hydrochloride shows the selective and concentration-dependent inhibition effects on bovine and human dopamine-beta-hydroxylase activity with IC50 of 8.5 nM and 9.0 nM, respectively. While Nepicastat hydrochloride has negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. [1] |
体内活性 | In the artery, left ventricle and cerebral cortex of spontaneously hypertensive rats (SHRs), Nepicastat hydrochloride reduces noradrenaline content, and increases dopamine content and dopamine/noradrenaline ratio in a dose-dependent manner. In addition, Nepicastat hydrochloride also produces the similar effects on noradrenaline, dopamine and dopamine/noradrenaline ratio in tissues and plasma of beagle dogs. [1] In inactin-anesthetized SHRs, Nepicastat hydrochloride (3 mg/kg, i.v.) produces the antihypertensive effects and causes a significant decrease in renal vascular resistance (38%) and an increase in renal blood flow (22%). [2] In dogs with chronic heart failure, low-dose Nepicastat hydrochloride (0.5 mg/kg) prevents left ventricular (LV) dysfunction and remodeling, and combination therapy of Nepicastat hydrochloride and enalapril results in additional improvements in all morphological features. [3] In rat brain, Nepicastat hydrochloride at a dose of 50 mg/kg ( i.p.) leads to the reduction of norepinephrine (NE) and blocks cocaine-primed reinstatement of cocaine seeking. [4] |
别名 | Nepicastat HCl, 内匹司他盐酸盐, RS-25560-197 hydrochloride, SYN-117 hydrochloride, Nepicastat (SYN-117) HCl |
分子量 | 331.81 |
分子式 | C14H15F2N3S·HCl |
CAS No. | 170151-24-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 33.2 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.0138 mL | 15.0689 mL | 30.1377 mL | 75.3443 mL |
5 mM | 0.6028 mL | 3.0138 mL | 6.0275 mL | 15.0689 mL | |
10 mM | 0.3014 mL | 1.5069 mL | 3.0138 mL | 7.5344 mL | |
20 mM | 0.1507 mL | 0.7534 mL | 1.5069 mL | 3.7672 mL | |
50 mM | 0.0603 mL | 0.3014 mL | 0.6028 mL | 1.5069 mL | |
100 mM | 0.0301 mL | 0.1507 mL | 0.3014 mL | 0.7534 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Nepicastat hydrochloride 170151-24-3 Metabolism Hydroxylase Dopamine beta-monooxygenase Dopamine beta-hydroxylase Dopamine β-monooxygenase Nepicastat SYN117 Nepicastat Hydrochloride SYN-117 Dopamine β-hydroxylase Inhibitor RS-25560-197 Hydrochloride SYN 117 Hydrochloride SYN 117 Nepicastat HCl inhibit 内匹司他盐酸盐 RS-25560-197 hydrochloride SYN-117 hydrochloride SYN117 Hydrochloride Nepicastat (SYN-117) HCl SYN-117 Hydrochloride inhibitor