Safinamide MesylateMAO-B inhibitor,potent,selective and reversible CAS# 202825-46-5 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| 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. |
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| 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. |
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| 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. | ||
| Description | Safinamide Mesylate is a potent and selective inhibitor of MAO-B with IC50 value of 98 nM. | |||||
| Targets | MAO-B | |||||
| IC50 | 98 nM | |||||
Safinamide Mesylate Dilution Calculator
Safinamide Mesylate Molarity Calculator
| 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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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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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.
