Raxatrigine
Based on 1 Customer Validation
Raxatrigine (GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
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- Pureté: 99.85%
- CAS No.: 934240-30-9
- Formule: C18H19FN2O2
- Masse moléculaire:314.35
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Membrane Transporter/Ion Channel Compound Library
HY-L011
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Clinical Compound Library
HY-L026
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Drug Repurposing Compound Library
HY-L035
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Neuroprotective Compound Library
HY-L070
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Sodium Channel Blocker Library
HY-L118
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Heterocyclic Compound Library
HY-L138
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Ion Channel Compound Library
HY-L166
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Drug Repurposing Compound Library Plus
HY-L035P
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Clinical Compound Library Plus
HY-L026P
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Activité biologique
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Nav1.7 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
10 μM
Compound: 2; BIIB074/CNV-1014802
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Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
13 μM
Compound: 2; BIIB074/CNV-1014802
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Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
15 μM
Compound: 2; BIIB074/CNV-1014802
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Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
22 μM
Compound: 2; BIIB074/CNV-1014802
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Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
23 μM
Compound: 2; BIIB074/CNV-1014802
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Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
32 μM
Compound: 2; BIIB074/CNV-1014802
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Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
6 μM
Compound: 2; BIIB074/CNV-1014802
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Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
84 μM
Compound: 2; BIIB074/CNV-1014802
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Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
Like lamotrigine, both GSK2 and GSK3 were able to prevent the deficit in reversal learning produced by PCP, thus confirming their potential in the treatment of cognitive symptoms of schizophrenia. However, higher doses than those required for anticonvulsant efficacy of the drugs were needed for activity in the reversal-learning model, suggesting a lower therapeutic window relative to mechanism-dependent central side effects for this indication. Raxatrigine (GSK-1014802) received orphan-drug designation from the US Food and Drug Administration in July 2013.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 934240-30-9
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Appearance Solid
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Masse moléculaire 314.35
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Formule C18H19FN2O2
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Color White to off-white
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SMILES
O=C([C@H]1N[C@@H](C2=CC=C(OCC3=CC=CC=C3F)C=C2)CC1)N
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Synonyms
Vixotrigine; GSK-1014802; CNV1014802
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (318.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (270 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1812 mL | 15.9058 mL | 31.8117 mL | 79.5292 mL |
| 5 mM | 0.6362 mL | 3.1812 mL | 6.3623 mL | 15.9058 mL | |
| 10 mM | 0.3181 mL | 1.5906 mL | 3.1812 mL | 7.9529 mL | |
| 15 mM | 0.2121 mL | 1.0604 mL | 2.1208 mL | 5.3019 mL | |
| 20 mM | 0.1591 mL | 0.7953 mL | 1.5906 mL | 3.9765 mL | |
| 25 mM | 0.1272 mL | 0.6362 mL | 1.2725 mL | 3.1812 mL | |
| 30 mM | 0.1060 mL | 0.5302 mL | 1.0604 mL | 2.6510 mL | |
| 40 mM | 0.0795 mL | 0.3976 mL | 0.7953 mL | 1.9882 mL | |
| 50 mM | 0.0636 mL | 0.3181 mL | 0.6362 mL | 1.5906 mL | |
| 60 mM | 0.0530 mL | 0.2651 mL | 0.5302 mL | 1.3255 mL | |
| 80 mM | 0.0398 mL | 0.1988 mL | 0.3976 mL | 0.9941 mL | |
| 100 mM | 0.0318 mL | 0.1591 mL | 0.3181 mL | 0.7953 mL |
Raxatrigine Related Classifications
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