中文名：Safinamide Mesylate
英文名：Safinamide Mesylate
英文别名：PNU-151774E,FCE28073;(S)-2-(4-(3-fluorobenzyloxy)benzylamino)propanamide,methanesulfonate
纯度：10mM in DMSO
货号：S408073
包装：1ml
Cas号：202825-46-5
存储温度：-80℃储存
产品介绍：
Information
Safinamide Mesylate (PNU-151774E, FCE28073) is mesylate salt of Safinamide, selectively and reversibly inhibitsMAO-BwithIC50of 98 nM, exhibits 5918-fold selectivity against MAO-A. Phase 3.
In vitro
Safinamide is a highly selective MAO-B inhibitor in rat brain mitochondria, with an IC50 of 98 nM. safinamide inhibits MAO-B in human brain with an IC50 of 9 nM. Safinamide has high affinity for the Na+ channel-binding site II in rat cortical membranes, with an IC50 of 8 μM. Safinamide inhibits the fast Na+ currents in a concentration- and state-dependent manner in rat cortical neurons. Safinamide blocks N-Type Ca2+ currents in rat cortical neurons with IC50 of 23 μM. Safinamide inhibits glutamate release induced by depolarizing conditions in rat hippocampal synaptosomes with IC50 of 9 μM. Safinamide incubated 1 hour before veratridine reduces the neuron damage with an IC50 1.4 μM through blockade of opening voltage-dependent Na+ and Ca2+ channels in rat primary cortical neurons. Safinamide binds to human MAO B with a Ki of 0.5 μM. Safinamide binds to human MAO B in an extended conformation occupying both flavin and entrance cavity.
In vivo
Safinamide orally administrated dose-dependently inhibits mouse brain MAO-B with IC50 of 0.6 mg/kg, and MAO-B activity recovers quickly, starting from 8 hours. Safinamide significantly 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 intraperitoneally administrated at dose of 100 mg/kg shows a relevant neurorescuing 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.
Cell Data
cell lines：U-937, HL-60, CRL-1872, ACHN, NCI-H226, Hs888Lu, Hs578Bst, MCF-10A, SK-MEL-5, BT-20, MDA-MB-231, UACC-62, SK-N-SH, B16-F10 , Hs 578t, and PC-12
Concentrations：
Incubation Time：
Powder Purity:≥99%
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关键字： PNU-151774E,FCE28073;(S)-2-(4-(3-fluorobenzyloxy)benzylamino)propanamide,methanesulfonate
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