化学性质
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 398.45 |
Cas No. | 202825-46-5 |
Formula | C17H19FN2O2·CH4O3S |
Synonyms | FCE-28073, PNU 151774E, methanesulfonate |
Solubility | ≥10.08 mg/mL in EtOH with gentle warming and ultrasonic; ≥16.1 mg/mL in DMSO; ≥84.6 mg/mL in H2O |
Chemical Name | (2S)-2-[[4-[(3-fluorophenyl)methoxy]phenyl]methylamino]propanamide;methanesulfonic acid |
Canonical SMILES | CC(C(=O)N)NCC1=CC=C(C=C1)OCC2=CC(=CC=C2)F.CS(=O)(=O)O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
资料参考
Safinamide Mesylate是活性组分safinamide的甲磺酸形式,Safinamide是选择性和可逆的单胺氧化酶B(MAO-B)抑制剂,IC50值为98 nM。Safinamide可以用于治疗帕金森氏病(PD),多巴胺是MAO-B的底物,safinamide强效调节多巴胺(DA),抑制多巴胺吸收,Safinamide与MAO-B可逆地结合,阻碍MAO-B的功能,进而缓解PD症状。除了抑制MAO-B外,Safinamide还具有一定的抗惊厥效果,可以作为钠通道、钙通道阻滞剂,抑制谷氨酸的释放,其IC50分别值8.2 μM,31.5 μM和大于56.4 μM。
参考文献:
Fariello RG, McArthur RA, Bonsignori A, Cervini MA, Maj R, Marrari P, Pevarello P, Wolf HH, Woodhead JW, White HS, Varasi M, Salvati P, Post C. Preclinical evaluation of PNU-151774E as a novel anticonvulsant. J Pharmacol Exp Ther. 1998; 285(2): 397-403
Onofrj M, Bonanni L, Thomas A. An expert opinion on safinamide in Parkinson's disease. Expert Opin Investig Drugs. 2008;17(7):1115-1125
Naveed M Malek, Donald G Grosset. Investigational agents in the treatment of Parkinson's disease: focus on safinamide. Journal of Experimental Pharmacology 2012: 4 85-90
生物活性
Description | Safinamide Mesylate(沙芬酰胺甲磺酸)是MAO-B的有效选择性抑制剂,IC50值为98 nM。 |
靶点 | MAO-B | | | | | |
IC50 | 98 nM | | | | | |