Safinamide mesylate

SKU: orb1222536

Description

Safinamide Mesylate, a mesylate salt of Safinamide, can reversibly and specifically inhibit MAO-B (IC50: 98 nM), has 5918-fold selectivity against MAO-A.(In Vitro):Safinamide mesylate (1-300 μM) reduces the amplitude of the peak sodium currents in a concentration-dependent manner. When currents are stimulated to a Vtest of +10 mV from a Vh of -110 mV, the IC50 value was 262 μM. When the holding potential is depolarized to -53 mV, the inhibitory effect of Safinamide mesylate with a lower IC50 value (8 μM) in rat cortical neurons.(In Vivo):Safinamide mesylate (intraperitoneal injection; 90 mg/kg; once daily; 14 days) treatment prior to MCAO significantly ameliorates MCAO-caused cerebral infarction volume, neurological deficit, disruption of the brain-blood barrier (BBB), and impairs expression of tight junction protein occludin and ZO-1 in mice.Safinamide mesylate (intraperitoneal injection; 5 mg/kg, 15 mg/kg and 30 mg/kg) dose dependently inhibits the veratridine-induced GABA release and Glu release in vivo. At the dose 30 mg/kg, Safinamide mesylate prevents the effect of veratridine both on Glu (treatment F1,8=1.31; time×treatment interaction F8,64=2.4) and GABA (treatment F1,8=4.04; time F8,64=3.76, time×treatment interaction F8,64=2.83) release.Safinamide mesylate causes a slight, albeit not significant, reduction of veratridine-stimulated Glu release at 0.5 mg/kg and full inhibition at 5 and 15 mg/kg in rat.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 202825-46-5
• MW: 398.45
• Purity: >98% (HPLC)
• Formula: C₁₈H₂₃FN₂O₅S
• SMILES: CS(=O)(=O)O.C[C@H](NCc1ccc(OCc2cc(F)ccc2)cc1)C(=O)N
• Target: Antifungal
• Solubility: In Vitro: DMSO : 250 mg/mL (627.43 mM)

Bioactivity

• In Vivo:
  Safinamide mesylate (intraperitoneal injection; 90 mg/kg; once daily; 14 days) treatment prior to MCAO significantly ameliorates MCAO-caused cerebral infarction volume, neurological deficit, disruption of the brain-blood barrier (BBB), and impairs expression of tight junction protein occludin and ZO-1 in mice. Safinamide mesylate (intraperitoneal injection; 5 mg/kg, 15 mg/kg and 30 mg/kg) dose dependently inhibits the veratridine-induced GABA release and Glu release In vivo. At the dose 30 mg/kg, Safinamide mesylate prevents the effect of veratridine both on Glu (treatment F1, 8 = 1.31; time×treatment interaction F8, 64 = 2.4) and GABA (treatment F1, 8 = 4.04; time F8, 64 = 3.76, time×treatment interaction F8, 64 = 2.83) release. Safinamide mesylate causes a slight, albeit not significant, reduction of veratridine-stimulated Glu release at 0.5 mg/kg and full inhibition at 5 and 15 mg/kg in rat.
• In Vitro:
  Safinamide mesylate (1-300 μM) reduces the amplitude of the peak sodium currents in a concentration-dependent manner. When currents are stimulated to a Vtest of +10 mV from a Vh of -110 mV, the IC50 value was 262 μM. When the holding potential is depolarized to -53 mV, the inhibitory effect of Safinamide mesylate with a lower IC50 value (8 μM) in rat cortical neurons.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Antifungal