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Safinamide Mesylate

Cat. No. M2006
Safinamide Mesylate Structure
Synonym:

FCE28073, PNU-151774E, NW-1015

Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 90  USD90 In stock
25mg USD 170  USD170 In stock
50mg USD 260  USD260 In stock
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Quality Control & Documentation
Biological Activity

Safinamide Mesylate is mesylate salt of Safinamide, which selectively and reversibly inhibits MAO-B with IC50 of 0.45 μM. Safinamide inhibits glutamate release induced by depolarizing conditions in rat hippocampal synaptosomes with IC50 of 9 μM. Safinamide increases neostriatal dopamine concentration. In addition, safinamide is voltage-dependent sodium and calcium channel blocker. Safinamide blocks N and L-type calcium channels and inhibits glutamate and aspartate release from synaptic terminals. Safinamide significantly inhibits cell body degeneration in the substantia nigra pars compacta. Safinamide has a high oral bioavailability (80–92%), is rapidly absorbed in plasma after reaching the peak within 0.5–2 hours declines, with a terminal half-life of about 3, 7, and 13 hours in mice, rats, and monkeys, respectively. Safinamide is currently in a Phase II clinical trial.

Chemical Information
Molecular Weight 398.45
Formula C17H19FN2O2.CH4O3S
CAS Number 202825-46-5
Solubility (25°C) DMSO 80 mg/mL
Water 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Michinori Koebisu, et al. Safinamide Mesilate (Equfina ® TABLETS 50 mg): preclinical and clinical pharmacodynamics, efficacy, and safety

[2] Daniel A Hussar, et al. Safinamide mesylate, Brodalumab, Guselkumab, and Abaloparatide

[3] Thomas Mller. Pharmacokinetic drug evaluation of safinamide mesylate for the treatment of mid-to-late stage Parkinson's disease

[4] Santiago Perez-Lloret, et al. The safety and efficacy of safinamide mesylate for the treatment of Parkinson's disease

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Keywords: Safinamide Mesylate, FCE28073, PNU-151774E, NW-1015 supplier, Monoamine Oxidase, inhibitors, activators


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