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Purity: ≥98%
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.
| ln Vitro |
The amplitude of peak sodium currents is lowered in a concentration-dependent manner by safinamide mesylate (1-300 µM). The IC50 value was 262 µM when currents were driven to a Vtest of +10 mV from a Vh of -110 mV. Rat cortical neurons have a depolarized holding potential of -53 mV due to the inhibitory effect of Safinamide mesylate, which has a lower IC50 value of 8 µM.
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| ln Vivo |
When administered intraperitoneally (90 mg/kg, once daily for 14 days), safinamide mesylate significantly reduces the volume of cerebral infarction caused by MCAO in mice, as well as the neurological deficit, disruption of the brain-blood barrier (BBB), and expression of ZO-1 and the tight junction protein occludin[3]. In vivo release of GABA and Glu is dose-dependently inhibited by safinamide mesylate (intraperitoneal injection; 5 mg/kg, 15 mg/kg, and 30 mg/kg). This effect is observed when veratridine is administered. Safinamide mesylate, at a dose of 30 mg/kg, blocks the effects of veratridine on the release of GABA (treatment F1,8=4.04; time F8,64=3.76, time×treatment interaction F8,64=2.83) and Glu (treatment F1,8=1.31; time×treatment interaction F8,64=2.4). In rats, safinamide mesylate completely inhibits veratridine-stimulated Glu release at doses of 5 and 15 mg/kg, while there is a minor but not statistically significant reduction at 0.5 mg/kg[3].
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| References |
[1]. Leonetti F, et al. Solid-phase synthesis and insights into structure-activity relationships of safinamide analogues as potent and selective inhibitors of type B monoamine oxidase. J Med Chem, 2007, 50(20), 4909-4916.
[2]. C Caccia, et al.Safinamide: from molecular targets to a new anti-Parkinson drug. Neurology. 2006 Oct 10;67(7 Suppl 2):S18-23. [3]. Michele Morari, et al. Safinamide Differentially Modulates In Vivo Glutamate and GABA Release in the Rat Hippocampus and Basal Ganglia.J Pharmacol Exp Ther. 2018 Feb;364(2):198-206. |
| Molecular Formula |
C17H19FN2O2.CH4O3S
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|---|---|
| Molecular Weight |
398.45
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| CAS # |
202825-46-5
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| Related CAS # |
Safinamide;133865-89-1
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| SMILES |
C[C@H](NCC1=CC=C(OCC2=CC=CC(F)=C2)C=C1)C(N)=O.CS(=O)(O)=O
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| Chemical Name |
(S)-2-((4-((3-fluorobenzyl)oxy)benzyl)amino)propanamide methanesulfonate
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| Synonyms |
PNU-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;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5097 mL | 12.5486 mL | 25.0973 mL | |
| 5 mM | 0.5019 mL | 2.5097 mL | 5.0195 mL | |
| 10 mM | 0.2510 mL | 1.2549 mL | 2.5097 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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