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Purity: ≥98%
Safinamide (formerly known as EMD-1195686; FCE-26743; EMD1195686; FCE26743; trade name: Xadago) is an FDA approved anti-PD ( Parkinson's disease) drug. It acts by selectively and reversibly inhibiting MAO-B with an IC50 of 98 nM, and exhibits 5918-fold selectivity against MAO-A. In addition, Safinamide is voltage-dependent sodium and calcium channel blocker. It appears to bind to the batrachotoxin-sensitive site 2 of the voltage-sensitive sodium channels. In 2017, FDA approved Safinamide to treat Parkinson's disease. Safinamide blocks N and L-type calcium channels and inhibits glutamate and aspartate release from synaptic terminals.
| ln Vitro |
Peak sodium current amplitude is lowered by safinamide (1–300 µM) in a concentration-dependent manner. The IC50 value was 262 µM when currents were driven to a Vtest of +10 mV from a Vh of -110 mV. In rat cortical neurons, safinamide exhibits an inhibitory action with a reduced IC50 value (8 µM) when the holding potential is depolarized to -53 mV[1].
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| ln Vivo |
When administered intraperitoneally (90 mg/kg, once daily for 14 days), safinamide significantly reduces the volume of cerebral infarction caused by MCAO in mice, as well as the neurological deficit, disruption of the blood-brain barrier (BBB), and expression of the tight junction proteins occludin and ZO-1[3]. In vivo, veratridine-induced GABA and Glu release is dose-dependently inhibited by safinamide (intraperitoneal injection; 5 mg/kg, 15 mg/kg, and 30 mg/kg). Safinamide blocks the effects of veratridine on 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) release at a dose of 30 mg/kg. In rats, safinamide completely inhibits veratridine-stimulated Glu release at doses of 5 and 15 mg/kg and reduces it slightly, but not significantly[3].
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| Animal Protocol |
Animal/Disease Models: Focal cerebral ischemia C57/BL6 male mouse Model[3]
Doses: 90 mg/kg Route of Administration: intraperitoneal (ip)injection; one time/day; 14 days Experimental Results: Dramatically diminished infarction volume in brain areas. |
| 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
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|---|---|
| Molecular Weight |
302.34
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| CAS # |
133865-89-1
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| Related CAS # |
Safinamide mesylate;202825-46-5;Safinamide-d4-1;2748522-33-8
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| SMILES |
C[C@H](NCC1=CC=C(OCC2=CC=CC(F)=C2)C=C1)C(N)=O
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| Chemical Name |
(S)-2-((4-((3-fluorobenzyl)oxy)benzyl)amino)propanamide
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| Synonyms |
PNU-151774E,FCE28073; EMD-1195686; EMD 1195686; FCE-26743; FCE 26743; FCE26743; EMD1195686; Safinamide. trade name: Xadago
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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) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3075 mL | 16.5377 mL | 33.0753 mL | |
| 5 mM | 0.6615 mL | 3.3075 mL | 6.6151 mL | |
| 10 mM | 0.3308 mL | 1.6538 mL | 3.3075 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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