Safinamide Mesylate|202825-46-5|(FCE 26743 mesylate; EMD 1195686 mesylate)-陌孚医药/Medlife

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Safinamide Mesylate (Synonyms: FCE 26743 mesylate; EMD 1195686 mesylate)

目录号: PC12518 纯度: ≥98%

CAS No. :202825-46-5

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中文名称	Safinamide Mesylate
中文别名	沙芬酰胺甲磺酸盐;甲磺酸沙芬酰胺
英文名称	Safinamide Mesylate
英文别名	(S)-2-((4-((3-Fluorobenzyl)oxy)benzyl)amino)propanamide methanesulfonate;(S)-( )-2-(4-(3-Fluorobenzyloxy) benzylamino)propanamide, methanesulfonate;NW 1015;(2R)-2-[[4-[(3-fluorophenyl)methoxy]phenyl]methylamino]propanamide;methanesulfonic acid;Propanamide, 2-(((4-((3-fluorophenyl)methoxy)phenyl)methyl)amino)-, (S)-, monomethanesulfonate;PNU 151774E;Safinamide mesylate;(S)-2-((4-((3-Fluorobenzyl)oxy)benzyl)-amino)propanamide methanesulfonate;Propanamide,2-[[[4-[(3-fluorophenyl)methoxy]- phenyl]methyl]amino]-,(2S)-,monomethanesulfonate;SAFINAMIDE MESILATE;Safinamide Methanesulfonate;FCE-26743;FCE-28073(R-isomer);N~2~-{4-[(3-fluorobenzyl)oxy]benzyl}-D-alaninamide methanesulfonate;NW-1015;PNU-151774E;(S)-2-[[4-[(3-Fluorobenzyl)oxy]benzyl]amino]propanamide methanesulfonate;(S)-(+)-2-[[4-(3-Fluorobenzoxy)benzyl]amino]propanamide;(S)-2-[[4-[(3-Fluorobenzyl)oxy]benzyl]amino]propanamide;PNU-151774E, NW-1015;Safinamide mesylate [USAN];YS90V3DTX0;Safinamide mesylate (USAN);R-isomer;Xadago (TN);Safi
Cas No.	202825-46-5
分子式	C₁₈H₂₃FN₂O₅S
分子量	398.45
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Safinamide (FCE 26743; EMD 1195686) mesylate is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC₅₀=0.098 μM) over MAO-A (IC₅₀=580 nM). Safinamide mesylate also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC₅₀=8 μM) than at resting (IC₅₀=262 μM) potentials. Safinamide mesylate has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke et.al.

性状

Solid

IC50 & Target[1][2]

MAO-B

98 nM (IC₅₀)

MAO-A

580 nM (IC₅₀)

体外研究(In Vitro)

Safinamide mesylate (1-300 μM) reduces the amplitude of the peak sodium currents in a concentration-dependent manner. When currents are stimulated to a V_test of +10 mV from a V_h of -110 mV, the IC₅₀ value was 262 μM. When the holding potential is depolarized to -53 mV, the inhibitory effect of Safinamide mesylate with a lower IC₅₀ value (8 μM) in rat cortical neurons.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Safinamide mesylate (intraperitoneal injection; 90 mg/kg; once daily; 14 days) treatment prior to MCAO significantly ameliorates MCAO-caused cerebral infarction volume, neurological deficit, disruption of the brain-blood barrier (BBB), and impairs expression of tight junction protein occludin and ZO-1 in mice.
Safinamide mesylate (intraperitoneal injection; 5 mg/kg, 15 mg/kg and 30 mg/kg) dose dependently inhibits the veratridine-induced GABA release and Glu release in vivo. At the dose 30 mg/kg, Safinamide mesylate prevents the effect of veratridine both on Glu (treatment F1,8=1.31; time×treatment interaction F8,64=2.4) and GABA (treatment F1,8=4.04; time F8,64=3.76, time×treatment interaction F8,64=2.83) release.
Safinamide mesylate causes a slight, albeit not significant, reduction of veratridine-stimulated Glu release at 0.5 mg/kg and full inhibition at 5 and 15 mg/kg in rat.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

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

ClinicalTrial

参考文献

[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. [Information]

[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. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 250 mg/mL (627.43 mM; Need ultrasonic)

H₂O : ≥ 20 mg/mL (50.19 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5097 mL	12.5486 mL	25.0972 mL
5 mM	0.5019 mL	2.5097 mL	5.0195 mL
10 mM	0.2510 mL	1.2549 mL	2.5097 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.22 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.22 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.22 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.22 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.22 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.22 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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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。

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