Home Metabolism MAO inhibitor Safinamide Mesylate

Safinamide Mesylate

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

For research use only.

Safinamide Mesylate (PNU-151774E, FCE28073) 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.

Safinamide Mesylate Chemical Structure

CAS No. 202825-46-5

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Biological Activity

Description Safinamide Mesylate (PNU-151774E, FCE28073) 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 (from reference)

Animal Research:

[2]
  • Animal Models: DA-depleted C57BL mice
  • Dosages: 20 mg/kg
  • Administration: Inject intraperitoneally in a single dose

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 398.45
Formula

C17H19FN2O2.CH4O3S
CAS No. 202825-46-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C(=O)N)NCC1=CC=C(C=C1)OCC2=CC(=CC=C2)F.CS(=O)(=O)O

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