Rufinamide-15N-d2 |
| رقم الكتالوجGC48895 |
An internal standard for the quantification of rufinamide
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1795037-48-7
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Canonical SMILES | FC1=C(C([2H])([2H])N2N=NC(C([15NH2])=O)=C2)C(F)=CC=C1 | ||
| Formula | C10H6D2F2N3[15N]O | M.Wt | 241.2 |
| الذوبان | Acetonitrile: slightly soluble,DMSO: slightly soluble | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.1459 mL | 20.7297 mL | 41.4594 mL |
| 5 mM | 829.2 μL | 4.1459 mL | 8.2919 mL |
| 10 mM | 414.6 μL | 2.073 mL | 4.1459 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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