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Nepicastat(SYN-117)HCl
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。
Nepicastat(SYN-117)HCl图片
CAS NO:170151-24-3
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)331.81
FormulaC14H15F2N3S.HCl
CAS No.170151-24-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 66 mg/mL (198.9 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES CodeS=C1NC=C(CN)N1[C@@H]2CC3=C(C(F)=CC(F)=C3)CC2.[H]Cl
SynonymsSYN117; RS25560197; RS25560-197; SYN-117; SYN 117; RS-25560-197; RS 25560-197; Nepicastat; Nepicastat HCl
实验参考方法
In Vitro

In vitro activity: 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.

In VivoIn 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. 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%). 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. 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.
Animal modelSpontaneously hypertensive rats (SHRs).
Formulation & DosageDissolved in distilled water; 100 mg/kg; p.o.
References

Br J Pharmacol. 1997 Aug;121(8):1803-9; J Cardiovasc Pharmacol. 1998 Jun;31(6):963-70.