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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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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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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation No information is available on the use of safinamide during breastfeeding. Because of liver toxicity in nursing rat pups, the manufacturer recommends that the drug not be used in nursing mothers. Alternate agents are preferred. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
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| References |
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| Additional Infomation |
See also: Safinamide (has active moiety).
Drug Indication Xadago is indicated for the treatment of adult patients with idiopathic Parkinson's disease (PD) as add-on therapy to a stable dose of Levodopa (L-dopa) alone or in combination with other PD medicinal products in mid-to late-stage fluctuating patients. |
| Molecular Formula |
C17H19FN2O2.CH4O3S
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|---|---|
| Molecular Weight |
398.45
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| Exact Mass |
398.131
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| CAS # |
202825-46-5
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| Related CAS # |
Safinamide;133865-89-1
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| PubChem CID |
3038502
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| Appearance |
White to off-white solid powder
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| Boiling Point |
476.7ºC at 760 mmHg
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| Melting Point |
210° (dec)
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| Flash Point |
242.1ºC
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| Vapour Pressure |
2.98E-09mmHg at 25°C
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| LogP |
4.044
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
438
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@@H](C(=O)N)NCC1=CC=C(C=C1)OCC2=CC(=CC=C2)F.CS(=O)(=O)O
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| InChi Key |
YKOCHIUQOBQIAC-YDALLXLXSA-N
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| InChi Code |
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-;/m0./s1
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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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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: ≥ 2.08 mg/mL (5.22 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 20.8 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: ≥ 2.08 mg/mL (5.22 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), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: Saline: 30 mg/mL |
| 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05312632 | Completed | Drug: Safinamide Mesilate | Parkinson Disease | Eisai Korea Inc. | April 5, 2022 | Phase 4 |
| NCT03753763 | Completed Has Results | Drug: Safinamide Methanesulfonate | Multiple System Atrophy | Zambon SpA | October 29, 2019 | Phase 2 |
| NCT03841604 | Completed Has Results | Drug: Safinamide Methanesulfonate | Idiopathic Parkinson Disease | Zambon SpA | April 9, 2019 | Phase 4 |
| NCT03987750 | Withdrawn | Drug: Safinamide Methanesulfonate 150mg |
Dyskinesia, Drug-Induced | Zambon SpA | October 2019 | Phase 3 |
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