Safinamide Mesylate

An inhibitor of MAO-B

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库存: 现货

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10mg

￥937.00

750.00

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50mg

￥3012.00

2410.00

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500mg

￥6625.00

5300.00

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货号: ajci13588
CAS: 202825-46-5
别名: 沙芬酰胺甲磺酸盐,FCE-28073, PNU 151774E, methanesulfonate
分子式: C17H19FN2O2.CH4O3S
分子量: 398.45
纯度: >98%
溶解度: ≥ 16.1 mg/mL in DMSO, ≥ 10.08 mg/mL in EtOH with ultrasonic and warming, ≥ 84.6 mg/mL in Water
储存: Store at -20°C
库存: 现货

Background

Safinamide mesylate is the methanesulfonic acid form of its active component safinamide, a selective and reversible monoamine oxidase B (MAO-B) inhibitor with the value of 50% inhibition concentration IC₅₀ of 98 nM. Having been used for the treatment of Parkinson’s disease (PD), safinamide potently modulates dopamine (DA), a substrate of MAO-B, suppressing DA uptake and reversibly binds to MAO-B blocking the function of MAO-B, which lead to the relief of PD symptoms. Besides MAO-B inhibition, safinamide exhibits novel anticonvulsant activities, including sodium channel blockade, calcium channel blockade and glutamate release inhibition, with values of IC₅₀ of 8.2 μM, 31.5 μM and >56.4 μM respectively.

Reference

[1].Fariello RG, McArthur RA, Bonsignori A, Cervini MA, Maj R, Marrari P, Pevarello P, Wolf HH, Woodhead JW, White HS, Varasi M, Salvati P, Post C. Preclinical evaluation of PNU-151774E as a novel anticonvulsant. J Pharmacol Exp Ther. 1998; 285(2): 397-403
[2].Onofrj M, Bonanni L, Thomas A. An expert opinion on safinamide in Parkinson's disease. Expert Opin Investig Drugs. 2008;17(7):1115-1125
[3].Naveed M Malek, Donald G Grosset. Investigational agents in the treatment of Parkinson's disease: focus on safinamide. Journal of Experimental Pharmacology 2012: 4 85-90