Safinamide mesylate

SKU: orb1300584

Description

Safinamide mesylate is a potent, reversible, and highly selective monoamine oxidase B (MAO-B) inhibitor, exhibiting an IC50 of 98 nM and >5,900-fold selectivity over MAO-A. It is widely used in research for investigating Parkinson's disease mechanisms and neuroprotection in both cellular and animal models.

Research Area

Metabolism Research, Neuroscience

Images & Validation

−

Key Properties

−

CAS Number	202825-46-5
MW	398.45
Purity	99.67%
Formula	C₁₈H₂₃FN₂O₅S
SMILES	CS(O)(=O)=O.C[C@H](NCc1ccc(OCc2cccc(F)c2)cc1)C(N)=O
Target	Monoamine Oxidase,MAO
Solubility	H2O:73 mg/mL (183.21 mM);DMSO:40 mg/mL (100.39 mM);Ethanol:11 mg/mL (27.61 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.02 mM)

Bioactivity

−

Target IC50	MAO-B:98 nM\|MAO-A:580 nM
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. Read more...
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. Read more...
Animal Research	Animal Models: DA-depleted C57BL miceFormulation: sterile 0.9% sodium chloride solutionDosages: 20 mg/kgAdministration: Inject intraperitoneally in a single dose Read more...

Storage & Handling

−

Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

−

deprivation/reperfusion, EMD1195686, EMD-1195686, EMD1195686 Mesylate, EMD-1195686 Mesylate, EMD 1195686, EMD 1195686 mesylate, FCE26743, FCE-26743, FCE28073 mesylate, FCE 26743, Glucose, MonoamineOxidase, Monoamine Oxidase, MAO, PNU-151774E,FCE 28073, PNU-151774E,FCE-28073, OGD/R, NW1015, NW 1015, neurorescuing, Parkinson, Stroke, Safinamide, α-aminoamide derivative

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID

3038502 ↗

Key Properties

−

No computed properties available.

Documents Download

Datasheet

Product Information

Download

Request a Document

Protocol Information

Find More Protocols