沙芬酰胺甲磺酸盐 T6651
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
1 mL | 202825-46-5 | ¥526.00 | 询底价 |
10 mg | 202825-46-5 | ¥667.00 | 询底价 |
50 mg | 202825-46-5 | ¥1,995.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Safinamide mesylate
描述: Safinamide mesylate (EMD 1195686 mesylate) 是选择性的、有效的、可逆的单胺氧化酶 B 的抑制剂,对 MAO-A 选择性较低。它能够阻断钠通道和调节谷氨酸释放。它具有神经保护作用,可用于研究帕金森病、缺血脑卒中等疾病。
动物实验: Animal Models: DA-depleted C57BL miceFormulation: sterile 0.9% sodium chloride solutionDosages: 20 mg/kgAdministration: Inject intraperitoneally in a single dose
体外活性: 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.
体内活性: 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.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: Ethanol : 11 mg/mL (27.6 mM)
DMSO : 74 mg/mL (185.7 mM)
H2O : 73 mg/mL (183.2 mM)
关键字: EMD 1195686 | Monoamine Oxidase | EMD-1195686 | EMD1195686 Mesylate | neuroprotective | EMD-1195686 Mesylate | NW 1015 | inhibit | OGD/R | NW1015 | Glucose | neurorescuing | Safinamide | Safinamide mesylate | anticonvulsant | MAO | PNU-151774E,FCE-28073 | deprivation/reperfusion | FCE-26743 | Safinamide Mesylate | FCE 26743 | Parkinson | PNU-151774E,FCE 28073 | α-aminoamide derivative | EMD1195686 | Stroke | FCE26743 | EMD 1195686 Mesylate | Inhibitor
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相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | ReFRAME Related Library | Drug-induced Liver Injury (DILI) Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Highly Selective Inhibitor Library | EMA Approved Drug Library | Target-Focused Phenotypic Screening Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途