Safinamide Mesylate

Catalog No.S1472 Synonyms: PNU-151774E,FCE28073

Safinamide Mesylate Chemical Structure

Molecular Weight(MW): 398.45

Safinamide Mesylate is mesylate salt of Safinamide, selectively and reversibly inhibits MAO-B with IC50 of 98 nM, exhibits 5918-fold selectivity against MAO-A. Phase 3.

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In DMSO USD 270 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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Biological Activity

Description Safinamide Mesylate is mesylate salt of Safinamide, selectively and reversibly inhibits MAO-B with IC50 of 98 nM, exhibits 5918-fold selectivity against MAO-A. Phase 3.
Features Greater than 5,000-fold potency in inhibiting MAO-B vs. MAO-A.
Targets
MAO-B [3]
()
98 nM
In vitro

Safinamide is a highly selective MAO-B inhibitor in rat brain mitochondria, with an IC50 of 98 nM. safinamide inhibits MAO-B in human brain with an IC50 of 9 nM. Safinamide has high affinity for the Na+ channel-binding site II in rat cortical membranes, with an IC50 of 8 μM. Safinamide inhibits the fast Na+ currents in a concentration- and state-dependent manner in rat cortical neurons. Safinamide blocks N-Type Ca2+ currents in rat cortical neurons with IC50 of 23 μM. Safinamide inhibits glutamate release induced by depolarizing conditions in rat hippocampal synaptosomes with IC50 of 9 μM. Safinamide incubated 1 hour before veratridine reduces the neuron damage with an IC50 1.4 μM through blockade of opening voltage-dependent Na+ and Ca2+ channels in rat primary cortical neurons. [1] Safinamide binds to human MAO B with a Ki of 0.5 μM. Safinamide binds to human MAO B in an extended conformation occupying both flavin and entrance cavity. [2]

In vivo Safinamide orally administrated dose-dependently inhibits mouse brain MAO-B with IC50 of 0.6 mg/kg, and MAO-B activity recovers quickly, starting from 8 hours. Safinamide significantly inhibits cell body degeneration in the substantia nigra pars compacta. Safinamide intraperitoneally administered 15 minutes before kainic acid protects against hippocampal neuron loss, starting at 10 mg/kg showing neuroprotective properties. Safinamide intraperitoneally administrated at dose of 100 mg/kg shows a relevant neurorescuing effect on hippocampal neurons when given 3 hours after ischemia. 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. [1]

Protocol

Animal Research:

[2]

+ Expand
  • Animal Models: DA-depleted C57BL mice
  • Formulation: sterile 0.9% sodium chloride solution
  • Dosages: 20 mg/kg
  • Administration: Inject intraperitoneally in a single dose
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 80 mg/mL (200.77 mM)
Water 80 mg/mL (200.77 mM)
Ethanol 13 mg/mL (32.62 mM)
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 398.45
Formula

C17H19FN2O2.CH4O3S

CAS No. 202825-46-5
Storage powder
in solvent
Synonyms PNU-151774E,FCE28073

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID