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首页 / 抑制剂/激动剂 / 神经信号通路 / MAO / Safinamide

沙芬酰胺 /Safinamide {[allProObj[0].p_purity_real_show]}

货号：A189271 同义名： FCE 26743;EMD 1195686

Safinamide is a reversible and highly selective MAO-B inhibitor with IC50 of 98 nM.

Safinamide 化学结构 CAS号：133865-89-1
Safinamide 化学结构
CAS号：133865-89-1
Safinamide 3D分子结构
CAS号：133865-89-1
Safinamide 化学结构 CAS号：133865-89-1
Safinamide 3D分子结构 CAS号：133865-89-1
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Safinamide 纯度/质量文件 产品仅供科研

货号：A189271 标准纯度： {[allProObj[0].p_purity_real_show]}
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产品名称 MAO ↓ MAO-A ↓ MAO-B ↓ 其他靶点 纯度
Sennoside A ++

MAO, IC50: 17 μM

 		98%+
Glycyrrhizic acid ++++

MAO, IC50: 0.16 μM

 		80% HPLC
Rasagiline ++++

MAO-A, IC50: 412 nM

 		++++

MAO-B, IC50: 4.43 nM

 		99+%
Isatin ++

MAO, IC50: 15 μM

 		+

MAO-A, IC50: 58 μM

 		++

MAO-B, IC50: 14 μM

 		98%
Paeonol +

MAO-A, IC50: 54.6 μM

 		+

MAO-B, IC50: 42.5 μM

 		98%
Tranylcypromine hydrochloride +++

MAO-A, IC50: 11.5 μM

 		+++

MAO-B, IC50: 7 μM

 		97%
Moclobemide +++

MAO-A (5-HT), IC50: 6.1 μM

 		99%+
Pargyline HCl ++

MAO-A, Ki: 13 μM

 		+++

MAO-B, Ki: 0.5 μM

 		99%+
Safinamide ++++

MAO-B, IC50: 98 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Safinamide 生物活性

靶点

  • MAO-B

    MAO-B, IC50:98 nM
描述 Glial cells contain two enzymes that metabolize biogenicamines: COMT and MAO. MAO, located in the outer mitochondrial membrane, occurs as two isozymes: A and B. MAO-A is predominantly found in the intestinal tract and, in the CNS, presynaptic neurons; MAO-B is mainly located in the brain, generally in glial cells near dopaminergic synapses. MAO-B regulates the free concentrations of biogenic amines in the synaptic cleft[3].Safinamide is a highly selective and reversible MAO-B inhibitor that produces an increase in extracellular levels of dopamine in the striatum[4]. The non-dopaminergic mechanism of action involves state- and use-dependent blockade of voltagegated sodium channels and modulation of N-type calcium channels, thereby inhibiting glutamate release[5]. In rats, safinamide was &5000-fold more potent in inhibiting MAO-B than MAO-A [6]. In humans, safinamide provided platelet MAO-B inhibition at doses of C0.5 mg/kg,but did not inhibit MAO-A enzyme activity at a dose of 10 mg/kg[7].Safinamide has demonstrated neuroprotective, neurorescuing, anti-inflammatory and tremorolytic properties in several animal models,and was shown to reduce the duration and intensity of levodopa-induced dyskinesia in parkinsonian monkeys[8]. in vitro , safinamide is not a substrate for the transporters P-glycoprotein, BCRP, OAT1B1, OAT1B3, OATP1A2 or OATP2B1. The metabolite safinamide acid is not a substrate for OCT2 or OAT1 but is a substrate for OAT3,although potential pharmacokinetic interactions are not likely to be clinically relevant. Safinamide acid does not inhibit OCT2, MATE1 or MATE2-K[9].

Safinamide 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00627640 Idiopathic Parkinson's Disease Phase 3 Completed - -
NCT00642889 Parkinson's Disease Phase 3 Completed - -
NCT01028586 Idiopathic Parkinson's Disease Phase 3 Terminated(Trial is terminated... 展开 >> due to a company decision to return all rights for Safinamide back to Newron Pharmaceuticals) 收起 << - Switzerland ... 展开 >> Enquire Central Contact Geneva, Switzerland 收起 <<

Safinamide 参考文献

[1]Binda C, Wang J, et al. Structures of human monoamine oxidase B complexes with selective noncovalent inhibitors: safinamide and coumarin analogs. J Med Chem. 2007 Nov 15;50(23):5848-52.

[2]Caccia C, Maj R, et al. Safinamide: from molecular targets to a new anti-Parkinson drug. Neurology. 2006 Oct 10;67(7 Suppl 2):S18-23.

[3] Bartl J,et al. Chronic monoamine oxidase-B inhibitor treatment blocks monoamine oxidase-A enzyme activity. J Neural Transm. 2014;121:379–83.

[4] Safinamide for Parkinson's disease. Drug Ther Bull. 2018 May;56(5):54-57.

[5] European Medicines Agency. Safinamide: summary of product characteristics. 2014.

[6] Caccia C, Maj R, Calabresi M, et al. Safinamide: from molecular targets to a new anti-Parkinson drug. Neurology. 2006;67(7 Suppl2):S18–23.

[7] Cattaneo C, Caccia C, Marzo A, et al. Pressor response to intravenous tyramine in healthy subjects after safinamide, a novel neuroprotectant with selective, reversible monoamine oxidase B inhibition. Clin Neuropharmacol. 2003;26(4):213–7

[8] Gregoire L, Jourdain VA, Townsend M, et al. Safinamide reduces dyskinesias and prolongs l-dopa antiparkinsonian effect in parkinsonian monkeys. Parkinsonism Relat Disord. 2013;19(5):508–14.

[9]European Medicines Agency. Xadago assessment report. 2014.

Safinamide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.31mL

0.66mL

0.33mL

16.54mL

3.31mL

1.65mL

33.08mL

6.62mL

3.31mL

Safinamide 技术信息

CAS号133865-89-1
分子式C17H19FN2O2
分子量 302.34
别名 FCE 26743;EMD 1195686;PNU-15774E
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C
溶解度

DMSO: 105 mg/mL(347.29 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Safinamide | FCE 26743;EMD 1195686;PNU-15774E | MAO | AmBeed-信号通路专用抑制剂 | Safinamide 纯度/质量文件 | Safinamide 亚型比较 | Safinamide 生物活性 | Safinamide 临床数据 | Safinamide 参考文献 | Safinamide 实验方案 | Safinamide 技术信息

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