| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Voltage-gated sodium channels Nav1.7 and Nav1.8.
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|---|---|
| ln Vitro |
Funapide is a potent inhibitor of voltage-gated sodium channels Nav1.7 and Nav1.8. It has IC50 values of 84 nM for Nav1.5 and 54 nM for Nav1.7. By blocking these channels, it reduces neuronal excitability and pain signaling in the peripheral nervous system.
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| ln Vivo |
In vivo, funapide is an orally active analgesic. It has been investigated for the treatment of various chronic pain conditions, including osteoarthritis, neuropathic pain, postherpetic neuralgia, and erythromelalgia. The compound's activity in the peripheral nervous system may reduce side effects associated with central nervous system-acting analgesics.
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| Enzyme Assay |
Sodium channel inhibition is assessed using in vitro electrophysiological assays, such as patch-clamp, on cells expressing Nav1.7 or Nav1.8 channels. The compound is applied at various concentrations, and the inhibition of sodium currents is measured. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular activity is evaluated in neurons or cell lines expressing Nav1.7 or Nav1.8 channels. Cells are treated with funapide, and sodium channel activity is measured by electrophysiology or using fluorescent membrane potential dyes. The compound's ability to inhibit neuronal excitability is assessed.
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| Animal Protocol |
In vivo efficacy is studied in animal models of chronic pain, such as models of neuropathic pain, inflammatory pain, or osteoarthritis. Funapide is administered orally, and pain responses are assessed using behavioral tests such as von Frey filaments, hot plate, or paw withdrawal latency. The compound's analgesic effects are evaluated.
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| ADME/Pharmacokinetics |
Funapide has a molecular formula of C22H14F3NO5 and a molecular weight of 429.34 g/mol. It is an orally active compound. The compound is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Specific toxicological data for funapide are available from clinical trials. As a sodium channel blocker, it may cause side effects such as dizziness, paresthesia, and headache. The compound is for research use and has been investigated in clinical trials.
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| References |
[2]. Recent progress\nin sodium channel modulators for pain. Bioorg Med Chem Lett. 2014 Aug\n15;24(16):3690-9. doi: 10.1016/j.bmcl.2014.06.038. Epub 2014 Jun 21. Review.\nPubMed PMID: 25060923. |
| Additional Infomation |
Funapide has been used in trials investigating pharmacokinetics, postherpetic neuralgia, and knee osteoarthritis.
Funapide (TV-45070, XEN402) is a research compound and a potent Nav1.7/1.8 inhibitor that has been investigated in clinical trials for chronic pain. It is not approved for clinical use. The compound is a small-molecule analgesic acting on peripheral sodium channels. |
| Molecular Formula |
C22H14F3NO5
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|---|---|
| Molecular Weight |
429.345
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| Exact Mass |
429.082
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| Elemental Analysis |
C, 61.54; H, 3.29; F, 13.27; N, 3.26; O, 18.63
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| CAS # |
1259933-16-8
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| Related CAS # |
(R)-Funapide;1259933-15-7
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| PubChem CID |
49836093
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.317
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
31
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| Complexity |
734
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1[C@]2(C3=CC=CC=C3N(C2=O)CC4=CC=C(O4)C(F)(F)F)C5=CC6=C(C=C5O1)OCO6
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| InChi Key |
NEBUOXBYNAHKFV-NRFANRHFSA-N
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| InChi Code |
InChI=1S/C22H14F3NO5/c23-22(24,25)19-6-5-12(31-19)9-26-15-4-2-1-3-13(15)21(20(26)27)10-28-16-8-18-17(7-14(16)21)29-11-30-18/h1-8H,9-11H2/t21-/m0/s1
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| Chemical Name |
(3'S)-1'-{[5-(trifluoromethyl)furan-2-yl]methyl}-2H,6H-spiro[furo[2,3-f][1,3]benzodioxole-7,3'-indol]-2'(1'H)-one
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| Synonyms |
TV-45070; TV 45070;
Funapide; 1259933-16-8; XEN402; Funapide, (+)-; XEN-401-S; TV45070; XEN402; XEN-402; XEN 402
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~465.82 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5.25 mg/mL (12.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 52.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5.25 mg/mL (12.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 52.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3291 mL | 11.6455 mL | 23.2910 mL | |
| 5 mM | 0.4658 mL | 2.3291 mL | 4.6582 mL | |
| 10 mM | 0.2329 mL | 1.1646 mL | 2.3291 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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