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Safinamide mesylate

Catalog No. T6651 CAS 202825-46-5

Synonyms: PNU-151774E,FCE28073, PNU-151774E, NW-1015, EMD 1195686 mesylate

Safinamide mesylate (EMD 1195686 mesylate) , a mesylate salt of Safinamide, can reversibly and specifically inhibit MAO-B (IC50: 98 nM), has 5918-fold selectivity against MAO-A.

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Safinamide mesylate, CAS 202825-46-5

Pack Size	Availability	Price/USD
2 mg	In stock	$ 36.00
5 mg	In stock	$ 56.00
10 mg	In stock	$ 81.00
25 mg	In stock	$ 152.00
50 mg	In stock	$ 234.00
100 mg	In stock	$ 304.00
1 mL * 10 mM (in DMSO)	In stock	$ 62.00

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Purity: 98.41%

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Description	Safinamide mesylate (EMD 1195686 mesylate) , a mesylate salt of Safinamide, can reversibly and specifically inhibit MAO-B (IC50: 98 nM), has 5918-fold selectivity against MAO-A.
Targets&IC50	MAO-B:98 nM
In vitro	Safinamide is a highly specific MAO-B inhibitor in rat brain mitochondria (IC50: 98 nM) and also inhibits MAO-B in human brain (IC50: 9 nM). Safinamide has a high affinity for the Na+ channel-binding site II in rat cortical membranes (IC50: 8 μM). Safinamide concentration- and state-dependently inhibits the fast Na+ currents in rat cortical neurons. Safinamide blocks N-Type Ca2+ currents in rat cortical neurons (IC50: 23 μM). Safinamide inhibits glutamate release induced by depolarizing conditions in rat hippocampal synaptosomes (IC50: 9 μM). Safinamide ( IC50: 1.4 μM) incubated 1 hour before veratridine reduces the neuron damage through blockade of opening voltage-dependent Na+ and Ca2+ channels in rat primary cortical neurons. Safinamide binds to human MAO-B (Ki: 0.5 μM). Safinamide binds to human MAO-B in an extended conformation occupying both flavin and entrance cavity.
In vivo	Safinamide (p.o.) dose-dependently inhibits mouse brain MAO-B (IC50: 0.6 mg/kg), and MAO-B activity recovers quickly, starting from 8 hours. Safinamide markedly 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 (100 mg/kg, i.p.) shows a relevant neuro rescuing 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.
Animal Research	Animal Models: DA-depleted C57BL miceFormulation: sterile 0.9% sodium chloride solutionDosages: 20 mg/kgAdministration: Inject intraperitoneally in a single dose

Synonyms	PNU-151774E,FCE28073, PNU-151774E, NW-1015, EMD 1195686 mesylate
Molecular Weight	398.45
Formula	C18H23FN2O5S
CAS No.	202825-46-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 11 mg/mL (27.6 mM)

DMSO: 74 mg/mL (185.7 mM)

H2O: 73 mg/mL (183.2 mM)

References and Literature

1. Caccia C, et al. Neurology, 2006, 67(7 Suppl 2), S18-23. 2. Binda C, et al. J Med Chem, 2007, 50(23), 5848-5852. 3. Leonetti F, et al. J Med Chem, 2007, 50(20), 4909-4916.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Inhibitor Library Highly Selective Inhibitor Library EMA Approved Drug Library Antidepressant Compound Library Fluorochemical Library Approved Drug Library Mitochondria-Targeted Compound Library Anti-Alzheimer's Disease Compound Library

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Related compounds with same targets

Allylthiourea (Z)-SU4312 PF-9601N Sennoside A AChE/BChE/MAO-B-IN-1 Ro 41-1049 hydrochloride Jatrorrhizine Tetrindole mesylate

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Keywords

Safinamide mesylate 202825-46-5 Metabolism Neuroscience MAO Monoamine Oxidase EMD 1195686 EMD-1195686 EMD1195686 Mesylate neuroprotective EMD-1195686 Mesylate PNU-151774E,FCE28073 NW 1015 PNU-151774E inhibit OGD/R NW1015 Glucose neurorescuing Safinamide anticonvulsant PNU-151774E,FCE-28073 deprivation/reperfusion FCE-26743 Safinamide Mesylate FCE 26743 Parkinson PNU-151774E,FCE 28073 α-aminoamide derivative NW-1015 EMD1195686 EMD 1195686 mesylate Stroke FCE26743 EMD 1195686 Mesylate Inhibitor inhibitor

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