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Safinamide Mesylate

MAO-B inhibitor,potent,selective and reversible CAS# 202825-46-5

Safinamide Mesylate

Catalog No. BCC2320----Order now to get a substantial discount!

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Chemical structure

Safinamide Mesylate

3D structure

Chemical Properties of Safinamide Mesylate

Cas No. 202825-46-5 SDF Download SDF
PubChem ID 5745209 Appearance Powder
Formula C18H23FN2O5S M.Wt 398.45
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO > 10 mM
Chemical Name (2R)-2-[[4-[(3-fluorophenyl)methoxy]phenyl]methylamino]propanamide;methanesulfonic acid
SMILES CC(C(=O)N)NCC1=CC=C(C=C1)OCC2=CC(=CC=C2)F.CS(=O)(=O)O
Standard InChIKey YKOCHIUQOBQIAC-UTONKHPSSA-N
Standard InChI InChI=1S/C17H19FN2O2.CH4O3S/c1-12(17(19)21)20-10-13-5-7-16(8-6-13)22-11-14-3-2-4-15(18)9-14;1-5(2,3)4/h2-9,12,20H,10-11H2,1H3,(H2,19,21);1H3,(H,2,3,4)/t12-;/m1./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Safinamide Mesylate

DescriptionSafinamide Mesylate is a potent and selective inhibitor of MAO-B with IC50 value of 98 nM.
TargetsMAO-B    
IC5098 nM     

Safinamide Mesylate Dilution Calculator

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Safinamide Mesylate Molarity Calculator

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Preparing Stock Solutions of Safinamide Mesylate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5097 mL 12.5486 mL 25.0973 mL 50.1945 mL 62.7431 mL
5 mM 0.5019 mL 2.5097 mL 5.0195 mL 10.0389 mL 12.5486 mL
10 mM 0.251 mL 1.2549 mL 2.5097 mL 5.0195 mL 6.2743 mL
50 mM 0.0502 mL 0.251 mL 0.5019 mL 1.0039 mL 1.2549 mL
100 mM 0.0251 mL 0.1255 mL 0.251 mL 0.5019 mL 0.6274 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Safinamide Mesylate

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

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

Onofrj M, Bonanni L, Thomas A. An expert opinion on safinamide in Parkinson's disease. Expert Opin Investig Drugs. 2008;17(7):1115-1125

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

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References on Safinamide Mesylate

The safety and efficacy of safinamide mesylate for the treatment of Parkinson's disease.[Pubmed:26849427]

Expert Rev Neurother. 2016;16(3):245-58.

Safinamide (brand name Xadago(R), Zambon S.p.A) is a third-generation reversible MAO-B inhibitor, which also blocks sodium voltage-sensitive channels and modulates stimulated release of glutamate. Safinamide was recently licensed by EMA for the treatment of PD as add-on therapy to a stable dose of levodopa alone or in combination with other PD medicinal products in mid-to advanced-stage fluctuating patients. It is also under review by the US FDA. Studies in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated monkeys and 6OHDA-lesioned rats suggest antiparkinsonian efficacy and antidyskinesic effects. Randomized, double-blind, placebo-controlled trials have shown efficacy for the treatment of motor symptoms in stable PD patients on dopamine agonists and in fluctuating PD patients on levodopa. Significant improvement in daily ON time was also observed in the latter. This effect was maintained for at least 2 years in double-blind conditions and, interestingly, without significant worsening of dyskinesia. Clinical studies have not detected any specific safety issue other than those already known with MAO-B inhibitors.

Description

Safinamide Mesylate is mesylate salt of Safinamide, selectively and reversibly inhibits MAO-B with IC50 of 98 nM, exhibits 5918-fold selectivity against MAO-A. Phase 3.

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