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  2. Neuronal Signaling
  3. Monoamine Oxidase
  4. Safinamide

Safinamide  (Synonyms: 沙芬酰胺; FCE 26743; EMD 1195686)

目錄號: HY-70057 純度: 99.89%
COA 產(chǎn)品使用指南 技術(shù)支持

Safinamide 是一種有效的、選擇性的、可逆的單胺氧化酶 B (MAO-B) 的抑制劑 (IC50=0.098 μM)，對 MAO-A (IC50=580 μM) 選擇性較低。Safinamide 也阻斷鈉通道和調(diào)節(jié)谷氨酸 (Glu) 釋放，在去極化時 (IC50= 8?μM) 比靜息電位 (IC50=262 μM) 時，顯示出更大的親和力。Safinamide 具有神經(jīng)保護(hù)作用，可用于帕金森病、缺血腦卒中等疾病的研究。

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Safinamide Chemical Structure

Safinamide Chemical Structure

CAS No. : 133865-89-1

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥330
In-stock
5 mg ￥300
In-stock
10 mg ￥420
In-stock
25 mg ￥720
In-stock
50 mg ￥1010
In-stock
100 mg ￥1420
In-stock
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Safinamide:

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)

查看 Monoamine Oxidase 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 μM) over MAO-A (IC50=580 μM)[1]. Safinamide 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 has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].

IC50 & Target[1]

MAO-B

98 nM (IC50)

MAO-A

580 μM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
BTI-TN-5B1-4 IC50
> 25900 nM
Compound: SAF
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method
[PMID: 31265934]
BTI-TN-5B1-4 IC50
0.0231 μM
Compound: Safinamide
Inhibition of human microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho
Inhibition of human microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho
[PMID: 31711793]
BTI-TN-5B1-4 IC50
23.07 nM
Compound: Safinamide
Inhibition of human microsomal MAO-B expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells assessed as reduction in H2O2 production using p-tyramine as substrate after 15 mins by fluorescence assay
Inhibition of human microsomal MAO-B expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells assessed as reduction in H2O2 production using p-tyramine as substrate after 15 mins by fluorescence assay
[PMID: 27244485]
BTI-TN-5B1-4 IC50
25900 nM
Compound: SAF
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay
[PMID: 30522087]
BTI-TN-5B1-4 IC50
5.18 nM
Compound: SAF
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method
[PMID: 31265934]
體外研究
(In Vitro)

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Safinamide (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[3].
Safinamide (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 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 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[3].

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

Animal Model: Focal cerebral ischemia C57/BL6 male mouse Model[3]
Dosage: 90 mg/kg
Administration: Intraperitoneal?injection; once daily; 14 days
Result: Significantly decreased infarction volume in brain areas.
Clinical Trial
分子量

302.34

Formula

C17H19FN2O2
CAS 號
性狀

固體

顏色

White to off-white

中文名稱

沙芬酰胺；沙非酰胺
運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實驗： 

DMSO 中的溶解度 : ≥ 100 mg/mL (330.75 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.3075 mL 16.5377 mL 33.0753 mL
5 mM 0.6615 mL 3.3075 mL 6.6151 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.27 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.27 mM); 懸濁液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.89%

參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3075 mL 16.5377 mL 33.0753 mL 82.6884 mL
5 mM 0.6615 mL 3.3075 mL 6.6151 mL 16.5377 mL
10 mM 0.3308 mL 1.6538 mL 3.3075 mL 8.2688 mL
15 mM 0.2205 mL 1.1025 mL 2.2050 mL 5.5126 mL
20 mM 0.1654 mL 0.8269 mL 1.6538 mL 4.1344 mL
25 mM 0.1323 mL 0.6615 mL 1.3230 mL 3.3075 mL
30 mM 0.1103 mL 0.5513 mL 1.1025 mL 2.7563 mL
40 mM 0.0827 mL 0.4134 mL 0.8269 mL 2.0672 mL
50 mM 0.0662 mL 0.3308 mL 0.6615 mL 1.6538 mL
60 mM 0.0551 mL 0.2756 mL 0.5513 mL 1.3781 mL
80 mM 0.0413 mL 0.2067 mL 0.4134 mL 1.0336 mL
100 mM 0.0331 mL 0.1654 mL 0.3308 mL 0.8269 mL
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產(chǎn)品名稱：
Safinamide
目錄號：
HY-70057
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