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Safinamide

Catalog No. T6651L   CAS 133865-89-1
Synonyms: EMD1195686, FCE26743, FCE 26743, EMD-1195686, EMD 1195686, FCE-26743

Safinamide (FCE-26743) is a reversible and selective monoamine oxidase B (IC50 0.098μM) inhibitor, reducing the degradation of dopamine, and a glutamate release inhibitor (IC50 8μM). It also inhibits dopamine reuptake. Safinamide also blocks sodium and calcium channels. Potential additional uses of Safinamide might be Parkinson's disease, restless leg syndrome and epilepsy.

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Safinamide Chemical Structure
Safinamide, CAS 133865-89-1
Pack Size Availability Price/USD Quantity
5 mg In stock $ 39.00
10 mg In stock $ 54.00
25 mg In stock $ 92.00
50 mg In stock $ 137.00
100 mg In stock $ 197.00
500 mg In stock $ 513.00
1 mL * 10 mM (in DMSO) In stock $ 46.00
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Purity: 99.9%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Safinamide (FCE-26743) is a reversible and selective monoamine oxidase B (IC50 0.098μM) inhibitor, reducing the degradation of dopamine, and a glutamate release inhibitor (IC50 8μM). It also inhibits dopamine reuptake. Safinamide also blocks sodium and calcium channels. Potential additional uses of Safinamide might be Parkinson's disease, restless leg syndrome and epilepsy.
Targets&IC50 MAO-A:580 μM, MAO-B:98 nM
In vitro Safinamide (1–300 µM) reduces the amplitude of the peak sodium currents in a concentration-dependent manner. 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].
In vivo Daily intraperitoneal injections of Safinamide 1mg/kg were administered for 14 days and the 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 (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 [2].
Synonyms EMD1195686, FCE26743, FCE 26743, EMD-1195686, EMD 1195686, FCE-26743
Molecular Weight 302.34
Formula C17H19FN2O2
CAS No. 133865-89-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (297.7 mM)

TargetMolReferences and Literature

1. Stocchi F, Torti M. Adjuvant therapies for Parkinson's disease: critical evaluation of safinamide. Drug Des Devel Ther. 2016 Feb 5;10:609-18. 2. Perez-Lloret S, Rascol O. The safety and efficacy of safinamide mesylate for the treatment of Parkinson's disease. Expert Rev Neurother. 2016;16(3):245-58. 3. Cattaneo C, et al. Safinamide as Add-On Therapy to Levodopa in Mid- to Late-Stage Parkinson's Disease Fluctuating Patients: Post hoc Analysesof Studies 016 and SETTLE. J Parkinsons Dis. 2016;6(1):165-7 4. Rasheed MZ, Tabassum H, Parvez S. Mitochondrial permeability transition pore: a promising target for the treatment of Parkinson's disease. Protoplasma. 2016 Jan 29.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Inhibitor Library Drug Repurposing Compound Library EMA Approved Drug Library Mitochondria-Targeted Compound Library Neuronal Signaling Compound Library Bioactive Compound Library FDA-Approved & Pharmacopeia Drug Library Bioactive Compounds Library Max Approved Drug Library

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Keywords

Safinamide 133865-89-1 Metabolism Neuroscience MAO EMD1195686 FCE26743 FCE 26743 EMD-1195686 EMD 1195686 FCE-26743 inhibitor inhibit

 

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