An inhibitor of MAO-B
Related Products
Isomer(s)
45954Ralfinamide (mesylate)
Labeled Version(s)
28490Safinamide-d4
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Safinamide (mesylate)

Item No. 21546

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2S-[[[4-[(3-fluorophenyl)methoxy]phenyl]methyl]amino]-propanamide, monomethanesulfonate
CAS Number
202825-46-5
Synonyms
  • EMD 1195686
  • FCE 26743
  • NW-1015
  • PNU-151774E
Molecular Formula
C17H19FN2O2 • CH3SO3H
Formula Weight
398.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2)(1:9): 0.1 mg/mlEthanol: 5 mg/mlPBS (pH 7.2): slightly soluble
λmax
228, 263, 269 nm
SMILES
FC1=CC(COC2=CC=C(CN[C@@H](C)C(N)=O)C=C2)=CC=C1.O=S(O)(C)=O
InChi Code
InChI=1S/C17H19FN2O2.CH4O3S/c1-12(17(19)21)20-10-13-5-7-16(8-6-13)22-11-14-3-2-4-15(18)9-14;1-5(2,3)4/h2-9,12,20H,10-11H2,1H3,(H2,19,21);1H3,(H,2,3,4)/t12-;/m0./s1
InChi Key
YKOCHIUQOBQIAC-YDALLXLXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $69

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    10 mg

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    25 mg

    $297

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    50 mg

    $558

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    Product Description

    Safinamide is an inhibitor of monoamine oxidase B (MAO-B; IC50 = ~0.1 μM).1 It is selective for MAO-B over MAO-A (IC50 = >10 μM). It also inhibits radioligand binding to sodium channel binding site 2, sigma-1, and sigma-2 receptors in rat brain membranes (IC50s = 8.2, 0.019, and 1.59 μM, respectively).2 Safinamide inhibits high voltage-activated calcium currents and depolarization-induced tetrodotoxin-sensitive fast sodium currents in rat hippocampal neurons in a concentration-dependent manner. It inhibits veratrine-induced glutamate release in rat hippocampal slices (IC50 = 56 μM). Safinamide inhibits maximal electroshock-induced tonic extension seizures in mice and rats (ED50s = 8 and 11.8 mg/kg, p.o.) as well as maximal seizures induced by bicuculline (Item No. 11727), picrotoxin (Item No. 20771), 3-mercaptopropionic acid, and strychnine in mice (ED50s = 26.9, 60.6, 21.5, and 104.1 mg/kg, p.o., respectively).3 Formulations containing safinamide have been used as adjunctive treatments to levodopa and carbidopa in the treatment of “off” episodes associated with Parkinson’s disease.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Strolin Benedetti, M.S., Marrari, P., Colombo, M., et al. The anticonvulsant FCE 26743 is a selective and short-acting MAO-B inhibitor devoid of inducing properties towards cytochrome P450-dependent testosterone hydroxylation in mice and rats. J. Pharm. Pharmacol. 46(10), 814-819 (1994).

    2. Salvati, P., Maj, R., Caccia, C., et al. Biochemical and electrophysiological studies on the mechanism of action of PNU-151774E, a novel antiepileptic compound. J. Pharmacol. Exp. Ther. 288(3), 1151-1159 (1999).

    3. Fariello, R.G., McArthur, R.A., Bonsignori, A., et al. Preclinical evaluation of PNU-151774E as a novel anticonvulsant. J. Pharmacol. Exp. Ther. 285(2), 397-403 (1998).