1. Neuronal Signaling
  2. Monoamine Oxidase
  3. Safinamide

Safinamide (Synonyms: FCE 26743; EMD 1195686)

Cat. No.: HY-70057 Purity: 99.95%
Handling Instructions

Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.

For research use only. We do not sell to patients.

Safinamide Chemical Structure

Safinamide Chemical Structure

CAS No. : 133865-89-1

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10 mM * 1 mL in DMSO USD 106 In-stock
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Description

Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].

IC50 & Target

MAO-B

98 nM (IC50)

MAO-A

580 μM (IC50)

In Vitro

Safinamide (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 with a lower IC50 value (8 µM) in rat cortical neurons[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Safinamide (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[3].
Safinamide (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 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 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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Focal cerebral ischemia C57/BL6 male mouse Model[3]
Dosage: 90 mg/kg
Administration: Intraperitoneal injection; once daily; 14 days
Result: Significantly decreased infarction volume in brain areas.
Clinical Trial
Molecular Weight

302.34

Formula

C₁₇H₁₉FN₂O₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (330.75 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3075 mL 16.5377 mL 33.0753 mL
5 mM 0.6615 mL 3.3075 mL 6.6151 mL
10 mM 0.3308 mL 1.6538 mL 3.3075 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (9.10 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.75 mg/mL (9.10 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (9.10 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.95%

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Safinamide
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