Safinamide mesylate - CAS:202825-46-5

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

目录号 : KM16642 CAS No. : 202825-46-5 纯度 : 98%

Data Sheet 产品使用指南

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) 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。

规格	价格	是否有货
10mg		In-stock
50mg		In-stock
100mg	询价	In-stock
200mg	询价	In-stock

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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.

体外研究

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.

体内研究

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.

分子式

C₁₈H₂₃FN₂O₅S

分子量

398.45

CAS号

202825-46-5

中文名称

沙芬酰胺甲磺酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

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)

溶解性数据

In Vitro:

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

H₂O : ≥ 20 mg/mL (50.19 mM)

配制储备液

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

请依序添加每种溶剂： 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。
2.

请依序添加每种溶剂： 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。
3.

请依序添加每种溶剂： 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。

临床试验

纯度： 98%

Data Sheet

产品使用指南

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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Other Forms of Rapamycin:

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