[CAS NO. 133865-89-1] Safinamide

Name: Safinamide
Brand: Arctom Scientific
SKU: SLK-S5357

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PRODUCTS SPECIFICATIONS [133865-89-1]

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Catalog

SLK-S5357

Brand

Selleck

CAS

133865-89-1

DESCRIPTION [133865-89-1]

Overview

MDL	MFCD00897036
Molecular Weight	302.34
Molecular Formula	C17H19FN2O2
SMILES	O(CC1=CC(F)=CC=C1)C2=CC=C(CN[C@H](C(N)=O)C)C=C2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume 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
50 mM	0.0662 mL	0.3308 mL	0.6615 mL

Description

Safinamide (EMD-1195686, PNU-15774E) is an orally active, selective, reversible

Targets

MAO-B ^[1]
(Microsomal)

16.7 nM(Ki)

In vitro

The antiparkinson mechanism of safinamide is through reversible inhibition of selective MAO-B, thus reducing the degradation of dopamine. It inhibits glutamate release and dopamine reuptake in the brain. Safinamide also blocks sodium and calcium channels.

In vivo

Safinamide is absorbed quickly, with a bioavailability of 95%, and a demonstrated time to maximum plasma concentration of 1.8-2.8 hours. It exhibits extensive extravascular distribution with a volume of distribution of approximately 165 L. Safinamide does not undergo significant first-pass metabolism and is mediated by amidase enzymes producing safinamide acid and other metabolites. Safinamide is mediated by cytochrome P450 (CYP) 3A4 isoenzymes. It is 88% to 90% plasma protein-bound and is primarily eliminated through the kidneys (approximately 76%) in the form of its metabolites, with an elimination half-life of 20 to 30 hours. About 1.5% of safinamide is found excreted in the feces. Safinamide exhibits linear pharmacokinetics after oral administration of 50 mg to 300 mg (three times the maximum recommended daily dose) with a steady state reached within five to six days.

References

[1] Rojas RJ, et al. Bioorg Med Chem. 2015, 23(4):770-8.
[2] Cruz MP. P T. 2017, 42(10):622-637.

Synonyms

Propanamide, 2-[[[4-[(3-fluorophenyl)methoxy]phenyl]methyl]amino]-, (2S)-

Propanamide, 2-[[[4-[(3-fluorophenyl)methoxy]phenyl]methyl]amino]-, (S)-

(2S)-2-[[[4-[(3-Fluorophenyl)methoxy]phenyl]methyl]amino]propanamide

FCE 26743

Safinamide

(S)-2-[[4-[(3-Fluorobenzyl)oxy]benzyl]amino]propanamide

EMD 1195686

(2S)-2-[[4-[(3-Fluorophenyl)methoxy]phenyl]methylamino]propanamide

(S)-2-[[[4-[(3-Fluorophenyl)methoxy]phenyl]methyl]amino]propanamide