您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Safinamide Mesylate
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Safinamide Mesylate
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。
Safinamide Mesylate图片
CAS NO:202825-46-5
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议
500mg电议

产品介绍
Safinamide (FCE 26743; EMD 1195686) mesylate 是一种有效的、选择性的、可逆的单胺氧化酶 B (MAO-B) 抑制剂 (IC50=0.098 μM),优于 MAO-A (IC50=580 nM)。
Cas No.202825-46-5
别名沙芬酰胺甲磺酸盐,FCE-28073, PNU 151774E, methanesulfonate
化学名(2S)-2-[[4-[(3-fluorophenyl)methoxy]phenyl]methylamino]propanamide;methanesulfonic acid
Canonical SMILESCC(C(=O)N)NCC1=CC=C(C=C1)OCC2=CC(=CC=C2)F.CS(=O)(=O)O
分子式C17H19FN2O2.CH4O3S
分子量398.45
溶解度≥ 16.1 mg/mL in DMSO, ≥ 10.08 mg/mL in EtOH with ultrasonic and warming, ≥ 84.6 mg/mL in Water
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Safinamide mesylate is the methanesulfonic acid form of its active component safinamide, a selective and reversible monoamine oxidase B (MAO-B) inhibitor with the value of 50% inhibition concentration IC50of 98 nM. Having been used for the treatment of Parkinson’s disease (PD), safinamide potently modulates dopamine (DA), a substrate of MAO-B, suppressing DA uptake and reversibly binds to MAO-B blocking the function of MAO-B, which lead to the relief of PD symptoms. Besides MAO-B inhibition, safinamide exhibits novel anticonvulsant activities, including sodium channel blockade, calcium channel blockade and glutamate release inhibition, with values of IC50of 8.2 μM, 31.5 μM and >56.4 μM respectively.

Reference

[1].Fariello RG, McArthur RA, Bonsignori A, Cervini MA, Maj R, Marrari P, Pevarello P, Wolf HH, Woodhead JW, White HS, Varasi M, Salvati P, Post C. Preclinical evaluation of PNU-151774E as a novel anticonvulsant. J Pharmacol Exp Ther. 1998; 285(2): 397-403
[2].Onofrj M, Bonanni L, Thomas A. An expert opinion on safinamide in Parkinson's disease. Expert Opin Investig Drugs. 2008;17(7):1115-1125
[3].Naveed M Malek, Donald G Grosset. Investigational agents in the treatment of Parkinson's disease: focus on safinamide. Journal of Experimental Pharmacology 2012: 4 85-90