Funapide
Based on 1 Customer Validation
Funapide (TV 45070; XEN402) is an orally active inhibitor of voltage-gated sodium channels (VGSC) in the peripheral nervous system with IC50 values ??of 84 nM and 54 nM for Nav1.5 and Nav1.7, respectively. Funapide has analgesic effects.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.83%
- CAS. Nr.: 1259933-16-8
- Formel: C22H14F3NO5
- Molecular Weight:429.35
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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Nav1.7 |
Nav1.8 |
Nav1.2 601 nM (IC50) |
Nav1.5 84 nM (IC50) |
Nav1.6 173 nM (IC50) |
Nav1.7 54 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.054 μM
Compound: 1;TV-45070/XEN-402
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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 |
0.084 μM
Compound: 1;TV-45070/XEN-402
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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] |
| HEK293 | IC50 |
0.17 μM
Compound: 1;TV-45070/XEN-402
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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 |
0.6 μM
Compound: 1;TV-45070/XEN-402
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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 |
4.8 μM
Compound: 1;TV-45070/XEN-402
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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] |
Funapide is a potent state-dependent voltage-gated sodium channel (VGSC) inhibitor with IC50s of 601, 84, 173 and 54 nM for NaV1.2, NaV1.5, NaV1.6 and NaV1.7, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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. Nr. 1259933-16-8
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Appearance Solid
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Molecular Weight 429.35
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Formel C22H14F3NO5
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Color Off-white to light yellow
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SMILES
O=C([C@]12COC3=C1C=C(OCO4)C4=C3)N(CC5=CC=C(C(F)(F)F)O5)C6=C2C=CC=C6
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Synonyms
TV 45070; XEN402
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 200 mg/mL (465.82 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 5.25 mg/mL (12.23 mM); Clear solution
This protocol yields a clear solution of ≥ 5.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (52.5 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.
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.
Reinheit & Dokumentation
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Data Sheet (281 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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Handling Instructions (2659 KB)
Verweise
[1]. Kitano Y, et al. Inhibition of NaV1.7: the possibility of ideal analgesics. RSC Med Chem. 2022 Aug 1;13(8):895-920. [Content Brief]
[2]. Price N , et al. Safety and Efficacy of a Topical Sodium Channel Inhibitor (TV-45070) in Patients With Postherpetic Neuralgia (PHN): A Randomized, Controlled, Proof-of-Concept, Crossover Study, With a Subgroup Analysis of the Nav1.7 R1150W Genotype. Clin J Pain. 2017 Apr;33(4):310-318. [Content Brief]
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 | 2.3291 mL | 11.6455 mL | 23.2910 mL | 58.2276 mL |
| 5 mM | 0.4658 mL | 2.3291 mL | 4.6582 mL | 11.6455 mL | |
| 10 mM | 0.2329 mL | 1.1646 mL | 2.3291 mL | 5.8228 mL | |
| 15 mM | 0.1553 mL | 0.7764 mL | 1.5527 mL | 3.8818 mL | |
| 20 mM | 0.1165 mL | 0.5823 mL | 1.1646 mL | 2.9114 mL | |
| 25 mM | 0.0932 mL | 0.4658 mL | 0.9316 mL | 2.3291 mL | |
| 30 mM | 0.0776 mL | 0.3882 mL | 0.7764 mL | 1.9409 mL | |
| 40 mM | 0.0582 mL | 0.2911 mL | 0.5823 mL | 1.4557 mL | |
| 50 mM | 0.0466 mL | 0.2329 mL | 0.4658 mL | 1.1646 mL | |
| 60 mM | 0.0388 mL | 0.1941 mL | 0.3882 mL | 0.9705 mL | |
| 80 mM | 0.0291 mL | 0.1456 mL | 0.2911 mL | 0.7278 mL | |
| 100 mM | 0.0233 mL | 0.1165 mL | 0.2329 mL | 0.5823 mL |
Funapide Related Classifications
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