Rufinamide-15N-d2
(Synonyms: [15N,2H2]-卢非酰胺) 目录号 : GC48895An internal standard for the quantification of rufinamide
Cas No.:1795037-48-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Rufinamide-15N-d2 is intended for use as an internal standard for the quantification of rufinamide by GC- or LC-MS. Rufinamide is an anticonvulsant.1 It inhibits the activation of voltage-gated sodium channel 1.1 (Nav1.1) when used at a concentration of 100 µM.2 Rufinamide inhibits Nav1.1, but not Nav1.2, Nav1.3, and Nav1.6, opening and increases the action potential threshold in primary rat hippocampal neurons. It is an inhibitor of carbonic anhydrase VA (CAVA; Ki = 343.8 nM) that is selective for CAVA over CAI and CAII (Kis = >10,000 nM for both).3 Rufinamide (100 µM) prolongs the preictal phase and reduces seizure-like event frequency in an in vitro model of epileptiform activity in rat hippocampal slices.4 It inhibits seizures induced by pentylenetetrazole in a mouse model of epilepsy (ED50 = 54 mg/kg, i.p.) and reduces kainic acid-induced neuronal cell death in the mouse hippocampal CA3 region when used at doses of 25, 50, and 100 mg/kg.5,6 Formulations containing rufinamide have been used in the treatment of seizures associated with Lennox-Gastaut Syndrome (LGS).
1.Wheless, J.W., and Vazquez, B.Rufinamide: A novel broad-spectrum antiepileptic drugEpilepsy Curr.10(1)1-6(2010) 2.Gilchrist, J.J., Dutton, S., Diaz-Bustamante, M., et al.Nav1.1 modulation by a novel triazole compound attenuates epileptic seizures in rodentsACS Chem. Biol.9(5)1204-1212(2014) 3.Costa, G., Carta, F., Ambrosio, F.A., et al.A computer-assisted discovery of novel potential anti-obesity compounds as selective carbonic anhydrase VA inhibitorsEur. J. Med. Chem.181111565(2019) 4.GÁll, Z., OrbÁn-Kis, K., and SzilÁgyi, T.Differential effects of sodium channel blockers on in vitro induced epileptiform activitiesArch. Pharm. Res.40(1)112-121(2017) 5.White, H.S., Franklin, M.R., Kupferberg, H.J., et al.The anticonvulsant profile of rufinamide (CGP 33101) in rodent seizure modelsEpilepsia49(7)1213-1220(2008) 6.Park, J.-A., and Lee, C.-H.Effect of Rufinamide on the kainic acid-induced excitotoxic neuronal death in the mouse hippocampusArch. Pharm. Res.41(7)776-783(2018)
Cas No. | 1795037-48-7 | SDF | |
别名 | [15N,2H2]-卢非酰胺 | ||
Canonical SMILES | FC1=C(C([2H])([2H])N2N=NC(C([15NH2])=O)=C2)C(F)=CC=C1 | ||
分子式 | C10H6D2F2N3[15N]O | 分子量 | 241.2 |
溶解度 | Acetonitrile: slightly soluble,DMSO: slightly soluble | 储存条件 | -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。 |
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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 | 4.1459 mL | 20.7297 mL | 41.4594 mL |
5 mM | 0.8292 mL | 4.1459 mL | 8.2919 mL |
10 mM | 0.4146 mL | 2.073 mL | 4.1459 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。
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