Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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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2 mg | 在庫あり | ¥ 8,500 | |||
5 mg | 在庫あり | ¥ 13,000 | |||
10 mg | 在庫あり | ¥ 18,500 | |||
25 mg | 在庫あり | ¥ 35,000 | |||
50 mg | 在庫あり | ¥ 54,000 | |||
100 mg | 在庫あり | ¥ 70,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 14,500 |
説明 | 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. |
ターゲット&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. |
動物実験 | Animal Models: DA-depleted C57BL miceFormulation: sterile 0.9% sodium chloride solutionDosages: 20 mg/kgAdministration: Inject intraperitoneally in a single dose |
別名 | PNU-151774E,FCE28073, PNU-151774E, NW-1015, EMD 1195686 mesylate |
分子量 | 398.45 |
分子式 | C18H23FN2O5S |
CAS No. | 202825-46-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 11 mg/mL (27.6 mM)
DMSO: 74 mg/mL (185.7 mM)
H2O: 73 mg/mL (183.2 mM)
You can also refer to dose conversion for different animals. 詳細
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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