CAS:202825-46-5
Storage:Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:HPLC≥98%
Appearance:White to off-white Solid
Safinamide mesylate 是一种有效的、选择性的、可逆的单胺氧化酶 B (MAO-B) 的抑制剂
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Safinamide mesylateCAS:202825-46-5
Storage:Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:HPLC≥98%
Appearance:White to off-white Solid
CAS | 202825-46-5 |
Chinese Name | 沙芬酰胺甲磺酸盐 |
English Name | Safinamide mesylate |
Synonyms | FCE26743mesylate;沙芬酰胺甲磺酸盐 |
Molecular Formula | C17H19FN2O2·CH4O3S |
Molecular Weight | 398.45 |
Solubility | Soluble in Water |
Purity | HPLC≥98% |
Appearance | White to off-white Solid |
Storage | Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
MDL | MFCD15145475 |
SMILES | C[C@H](NCC1=CC=C(OCC2=CC=CC(F)=C2)C=C1)C(N)=O.CS(=O)(O)=O |
Target Point | MAO-B |
Passage | Neuronal Signaling |
Background | Safinamide mesylate is a potent, selective, and reversible inhibitor of monoamine oxidase B (MAO-B) |
Biological Activity | Safinamide mesylate 是一种有效的、选择性的、可逆的单胺氧化酶 B (MAO-B) 的抑制剂 (IC50=0.098 μM),对 MAO-A (IC50=580 μM) 选择性较低。Safinamide mesylate 也阻断钠通道和调节谷氨酸 (Glu) 释放,在去极化时 (IC50= 8 μM) 比静息电位 (IC50=262 μM) 时,显示出更大的亲和力。Safinamide mesylate 具有神经保护作用,可用于帕金森病、缺血脑卒中等疾病的研究。[1-3] |
IC50 | MAO-B:98nM;mAO-A:580nM [1-3] |
In Vitro | 甲磺酸沙芬酰胺(1-300μM)以浓度依赖的方式降低钠电流峰值的振幅。当电流从-110 mV的Vh刺激到+10 mV的Vtest时,IC50值为262μM。当保持电位被去极化至-53 mV时,具有较低IC50值的甲磺酸沙芬酰胺的抑制作用(8μM)大鼠皮质神经元[1]。 |
In Vivo | 甲磺酸沙非那胺(腹腔注射;90mg/kg;每日一次;14天)在MCAO前治疗可显著改善MCAO引起的脑梗死体积、神经功能缺损、脑血屏障(BBB)的破坏,并降低小鼠紧密连接蛋白闭塞素和ZO-1的表达[3]。甲磺酸沙非那胺(腹腔注射:5mg/kg、15mg/kg和30mg/kg)剂量依赖性地抑制维拉替啶诱导的GABA和Glu释放。在剂量为30 mg/kg时,甲磺酸沙非那胺可阻止藜芦碱对Glu(治疗F1,8=1.31;时间×处理交互作用F8,64=2.4)和GABA(处理F1,8=4.04;时间F8,64=3.76,时间×处理交互作用F8,64=2.83)释放的影响。5 mg/kg剂量时,三甲基甲磺酸钠(5 mg/kg)对大鼠无明显抑制作用[5 mg/kg时,三甲基甲磺酸钠未引起明显的抑制作用。 |
Data Literature Source | [1]. Leonetti F,et al. Solid-phase synthesis and insights into structure-activity relationships of safinamide analogues as potent and selective inhibitors of type B monoamine oxidase. J Med Chem,2007,50(20),4909-4916. [2]. C Caccia,et al.Safinamide: from molecular targets to a new anti-Parkinson drug. Neurology. 2006 Oct 10;67(7 Suppl 2):S18-23. [3]. Michele Morari,et al. Safinamide Differentially Modulates In Vivo Glutamate and GABA Release in the Rat Hippocampus and Basal Ganglia.J Pharmacol Exp Ther. 2018 Feb;364(2):198-206. |
Unit | Bottle |
Specification | 5mg 10mg 50mg |
Safinamide mesylate 是一种有效的、选择性的、可逆的单胺氧化酶 B (MAO-B) 的抑制剂