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    Safinamide Mesylate
    Safinamide Mesylate

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0901
    CAS #: 202825-46-5Purity ≥98%

    Description: Safinamide Mesylate (formerly PNU-151774E, FCE-28073; NW-1015; EMD-1195686; Xadago), the mesylate salt of Safinamide, is a selective and reversible inhibitor of MAO-B with anti-PD (Parkinson's diseas) effects. In inhibits MAO-B with an IC50 of 98 nM, and exhibits 5918-fold selectivity for MAO-B over MAO-A. Safinamide mesylate is the 3rd generation reversible MAO-B inhibitor, which also blocks sodium voltage-sensitive channels and modulates stimulated release of glutamate. Safinamide (formerly known as EMD 1195686 and FCE 26743; trade name: Xadago) is an FDA approved drug. As of 2017, Safinamide gained FDA approval to treat Parkinson's disease. 

    References: Neurology. 2006 Oct 10;67(7 Suppl 2):S18-23; J Med Chem. 2007 Nov 15;50(23):5848-52. 

    Related CAS: 202825-46-5 (mesylate); 133865-89-1 (free base);

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    Molecular Weight (MW)398.45
    FormulaC17H19FN2O2.CH4O3S
    CAS No.202825-46-5; 133865-89-1 (free base);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 80 mg/mL (200.8 mM)
    Water: 80 mg/mL (200.8 mM) 
    Ethanol: 13 mg/mL (32.62 mM) 
    Solubility (In vivo)Saline: 30 mg/mL  
    SynonymsPNU-151774E, FCE28073; Safinamide mesylate; Xadago; NW 1015; PNU 151774E; EMD 1195686; FCE-28073; Safinamide mesilate; FCE 28073; NW1015; NW-1015; EMD-1195686; EMD1195686; PNU-151774E; 

    Chemical Name: (S)-2-((4-((3-fluorobenzyl)oxy)benzyl)amino)propanamide methanesulfonate

    SMILES Code: C[[email protected]](NCC1=CC=C(OCC2=CC=CC(F)=C2)C=C1)C(N)=O.CS(=O)(O)=O           


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    In Vitro

    In vitro activity: Safinamide is a highly selective MAO-B inhibitor in rat brain mitochondria, with an IC50 of 98 nM. safinamide inhibits MAO-B in human brain with an IC50 of 9 nM. Safinamide has high affinity for the Na+ channel-binding site II in rat cortical membranes, with an IC50 of 8 μM. Safinamide inhibits the fast Na+ currents in a concentration- and state-dependent manner in rat cortical neurons. Safinamide blocks N-Type Ca2+ currents in rat cortical neurons with IC50 of 23 μM. Safinamide inhibits glutamate release induced by depolarizing conditions in rat hippocampal synaptosomes with IC50 of 9 μM. Safinamide incubated 1 hour before veratridine reduces the neuron damage with an IC50 1.4 μM through blockade of opening voltage-dependent Na+ and Ca2+ channels in rat primary cortical neurons. Safinamide binds to human MAO B with a Ki of 0.5 μM. Safinamide binds to human MAO B in an extended conformation occupying both flavin and entrance cavity.


    Kinase Assay: Safinamide (EMD 1195686; FCE 26743) selectively and reversibly inhibits MAO-B with IC50 of 98 nM, exhibits 5918-fold selectivity against MAO-A.


    Cell Assay: Safinamide has high affinity for the Na+ channel-binding site II in rat cortical membranes, with an IC50 of 8 μM. Safinamide inhibits the fast Na+currents in a concentration- and state-dependent manner in rat cortical neurons. Safinamide blocks N-Type Ca2+ currents in rat cortical neurons with IC50 of 23 μM. Safinamide inhibits glutamate release induced by depolarizing conditions in rat hippocampal synaptosomes with IC50 of 9 μM. Safinamide incubated 1 hour before veratridine reduces the neuron damage with an IC50 1.4 μM through blockade of opening voltage-dependent Na+ and Ca2+channels in rat primary cortical neurons. Safinamide binds to human MAO B with a Ki of 0.5 μM. Safinamide binds to human MAO B in an extended conformation occupying both flavin and entrance cavity.

    In VivoSafinamide orally administrated dose-dependently inhibits mouse brain MAO-B with IC50 of 0.6 mg/kg, and MAO-B activity recovers quickly, starting from 8 hours. Safinamide significantly inhibits cell body degeneration in the substantia nigra pars compacta. Safinamide intraperitoneally administered 15 minutes before kainic acid protects against hippocampal neuron loss, starting at 10 mg/kg showing neuroprotective properties. Safinamide intraperitoneally administrated at dose of 100 mg/kg shows a relevant neurorescuing effect on hippocampal neurons when given 3 hours after ischemia. Safinamide has a high oral bioavailability (80-92%), is rapidly absorbed in plasma after reaching the peak within 0.5-2 hours declines, with a terminal half-life of about 3, 7, and 13 hours in mice, rats, and monkeys, respectively.
    Animal modelDA-depleted C57BL mice 
    Formulation & DosageDissolved in 0.9% sodium chloride solution; 20 mg/kg; i.p. injection 
    ReferencesNeurology. 2006 Oct 10;67(7 Suppl 2):S18-23; J Med Chem. 2007 Nov 15;50(23):5848-52. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     
    Safinamide Mesylate
    Structures of human monoamine oxidase B (MAO B) in complex with safinamide and two coumarin derivatives, all sharing a common benzyloxy substituent, were determined by X-ray crystallography. J Med Chem. 2007 Nov 15;50(23):5848-52. 



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