Safinamide Mesylate
(Synonyms: 沙芬酰胺甲磺酸盐,FCE-28073, PNU 151774E, methanesulfonate) 目录号 : GC14673An inhibitor of MAO-B
Cas No.:202825-46-5
Sample solution is provided at 25 µL, 10mM.
Safinamide mesylate is the methanesulfonic acid form of its active component safinamide, a selective and reversible monoamine oxidase B (MAO-B) inhibitor with the value of 50% inhibition concentration IC50 of 98 nM. Having been used for the treatment of Parkinson’s disease (PD), safinamide potently modulates dopamine (DA), a substrate of MAO-B, suppressing DA uptake and reversibly binds to MAO-B blocking the function of MAO-B, which lead to the relief of PD symptoms. Besides MAO-B inhibition, safinamide exhibits novel anticonvulsant activities, including sodium channel blockade, calcium channel blockade and glutamate release inhibition, with values of IC50 of 8.2 μM, 31.5 μM and >56.4 μM respectively.
Reference
[1].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
[2].Onofrj M, Bonanni L, Thomas A. An expert opinion on safinamide in Parkinson's disease. Expert Opin Investig Drugs. 2008;17(7):1115-1125
[3].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
Cas No. | 202825-46-5 | SDF | |
别名 | 沙芬酰胺甲磺酸盐,FCE-28073, PNU 151774E, methanesulfonate | ||
化学名 | (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 | ||
分子式 | C17H19FN2O2.CH4O3S | 分子量 | 398.45 |
溶解度 | ≥ 16.1 mg/mL in DMSO, ≥ 10.08 mg/mL in EtOH with ultrasonic and warming, ≥ 84.6 mg/mL in Water | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.5097 mL | 12.5486 mL | 25.0973 mL |
5 mM | 0.5019 mL | 2.5097 mL | 5.0195 mL |
10 mM | 0.251 mL | 1.2549 mL | 2.5097 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet