| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Nav1.7
Voltage-gated sodium channels (VGSC), primarily Nav1.7 and Nav1.8, with much lower potency than the (S)-enantiomer. |
|---|---|
| ln Vitro |
(R)-Funapide is the less active R-enantiomer of the potent Nav1.7 blocker Funapide. While the (S)-enantiomer has an IC50 of 1.5 nM for Nav1.7, the (R)-enantiomer is significantly less potent, with an IC50 of 131 uM (approximately 87,000-fold less active).
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| ln Vivo |
No specific in vivo data is available for the less active R-enantiomer. In vivo studies would use the more active (S)-Funapide to explore analgesic efficacy. The R-enantiomer is primarily used as a negative control to confirm that effects are due to target engagement.
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| Enzyme Assay |
Recombinant human Nav1.7 channels are expressed in HEK293 cells. Whole-cell patch-clamp recordings are performed. (R)-Funapide is applied at varying concentrations, and its IC50 for sodium current inhibition is calculated. This IC50 is typically in the micromolar range (131 uM), much higher than the active (S)-enantiomer.
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| Cell Assay |
HEK293 cells expressing human Nav1.7 channels are cultured in DMEM with 10% FBS. Whole-cell patch-clamp electrophysiology is performed. (R)-Funapide is applied at concentrations ranging from 0.1 to 1000 uM. The reduction in sodium current is measured, and the IC50 is determined from the dose-response curve.
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| Animal Protocol |
No in vivo studies are typically performed with the less active R-enantiomer. For the active (S)-enantiomer, it is formulated in a suitable vehicle and administered to rats or mice to assess analgesic activity in models like the formalin test, CFA-induced hyperalgesia, or nerve injury models.
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| ADME/Pharmacokinetics |
No specific PK data is available for the R-enantiomer. However, the more active (S)-enantiomer has good oral bioavailability and half-life. As a structural isomer, (R)-Funapide may have a similar PK profile but is unlikely to be used in vivo due to its low potency.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for the R-enantiomer. The active (S)-enantiomer Funapide is generally well-tolerated, with the main risk being loss of pain sensation and potential off-target CNS effects like dizziness or ataxia.
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| References | |
| Additional Infomation |
(R)-Funapide is the R-enantiomer of the potent Nav1.7 blocker Funapide. It is used as a research tool to study the structure-activity relationship (SAR) and the importance of chirality in sodium channel inhibition.
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| Molecular Formula |
C22H14F3NO5
|
|---|---|
| Molecular Weight |
429.34547662735
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| Exact Mass |
429.082
|
| CAS # |
1259933-15-7
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| Related CAS # |
Funapide;1259933-16-8
|
| PubChem CID |
58224170
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| Appearance |
White to light yellow solid powder
|
| LogP |
3.5
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
31
|
| Complexity |
734
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
FC(C1=CC=C(CN2C3C=CC=CC=3[C@]3(C2=O)COC2C=C4C(=CC3=2)OCO4)O1)(F)F
|
| InChi Key |
NEBUOXBYNAHKFV-OAQYLSRUSA-N
|
| 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-/m1/s1
|
| Chemical Name |
(7R)-1'-[[5-(trifluoromethyl)furan-2-yl]methyl]spiro[6H-furo[2,3-f][1,3]benzodioxole-7,3'-indole]-2'-one
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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: 220 mg/mL (512.40 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (11.65 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 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 mg/mL (11.65 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (11.65 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| 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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