| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
NaV1.7 inhibitor-1 targets the voltage-gated sodium channel NaV1.7, a key mediator of pain signaling in peripheral sensory neurons. By blocking NaV1.7, the compound reduces sodium influx, neuronal excitability, and pain-related peripheral sensory nerve signaling. It exhibits high selectivity for NaV1.7 over other sodium channel isoforms.
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| ln Vitro |
NaV1.7 inhibitor-1 potently blocks human NaV1.7 with an IC50 of 0.6 nM. It exhibits 80-fold selectivity over human NaV1.5, a cardiac sodium channel, minimizing off-target cardiovascular effects. The compound is a highly potent and selective inhibitor of the NaV1.7 channel with excellent in vitro potency in the sub-nanomolar range.
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| ln Vivo |
NaV1.7 inhibitor-1 has demonstrated efficacy in preclinical pain models by selectively blocking NaV1.7 channels, reducing sodium influx and neuronal excitability in peripheral sensory nerves. The compound's high potency (IC50 = 0.6 nM) and selectivity over hNaV1.5 make it a promising candidate for pain research and therapeutic development.
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| Enzyme Assay |
For NaV1.7 channel inhibition assays, HEK293 cells expressing human NaV1.7 are used in automated patch-clamp electrophysiology systems. Cells are treated with varying concentrations of NaV1.7 inhibitor-1, and sodium currents are recorded. IC50 values are calculated from dose-response inhibition curves. Selectivity over NaV1.5 is determined similarly using cells expressing human NaV1.5.
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| Cell Assay |
Cellular assays are performed using HEK293 or CHO cells stably expressing human NaV1.7 channels. Cells are treated with NaV1.7 inhibitor-1 at various concentrations, and sodium channel activity is measured by fluorescence-based membrane potential assays or automated patch-clamp electrophysiology. Inhibition of sodium influx is calculated from the reduction in fluorescence or current amplitude.
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| Animal Protocol |
In vivo efficacy is evaluated in rodent models of pain, such as the formalin test, complete Freund's adjuvant (CFA)-induced inflammatory pain, or spinal nerve ligation (SNL)-induced neuropathic pain. NaV1.7 inhibitor-1 is administered via appropriate routes (typically oral or intraperitoneal), and pain-related behaviors (e.g., paw withdrawal latency, mechanical allodynia) are assessed. Plasma and tissue concentrations are measured to establish pharmacokinetic-pharmacodynamic relationships.
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| ADME/Pharmacokinetics |
As a small molecule with a molecular weight of 435.55, NaV1.7 inhibitor-1 is likely to have good oral bioavailability and blood-brain barrier penetration. The compound's aryl sulfonamide structure suggests moderate lipophilicity and metabolic stability. Pharmacokinetic parameters such as half-life, clearance, and volume of distribution are determined in preclinical species following oral and intravenous administration.
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| Toxicity/Toxicokinetics |
NaV1.7 inhibitor-1 has demonstrated a favorable safety profile in preclinical studies with high selectivity over hNaV1.5 (80-fold), reducing the risk of cardiovascular side effects. The compound is well-tolerated at effective doses in animal models.
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| References | |
| Additional Infomation |
NaV1.7 inhibitor-1 is a potent and selective voltage-gated sodium channel NaV1.7 inhibitor with an IC50 of 0.6 nM for hNaV1.7 and 80-fold selectivity over hNaV1.5. It is an aryl sulfonamide small molecule that blocks NaV1.7 to reduce pain-related peripheral sensory nerve signaling.
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| Molecular Formula |
C23H30FNO4S
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|---|---|
| Molecular Weight |
435.55
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| Exact Mass |
435.187
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| CAS # |
1494585-79-3
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| PubChem CID |
90026208
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| Appearance |
White to off-white solid powder
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| LogP |
5.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
772
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(NS(C1CC1)(=O)=O)(=O)C1=CC(C2CC2)=C(OCC2(C)CCC3(CC3)CC2)C=C1F
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| InChi Key |
GFDXIUXAFNREKM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H30FNO4S/c1-22(6-8-23(9-7-22)10-11-23)14-29-20-13-19(24)18(12-17(20)15-2-3-15)21(26)25-30(27,28)16-4-5-16/h12-13,15-16H,2-11,14H2,1H3,(H,25,26)
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| Chemical Name |
5-cyclopropyl-N-cyclopropylsulfonyl-2-fluoro-4-[(6-methylspiro[2.5]octan-6-yl)methoxy]benzamide
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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 : ~100 mg/mL (~229.59 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.74 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.74 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 25.0 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 | 2.2959 mL | 11.4797 mL | 22.9595 mL | |
| 5 mM | 0.4592 mL | 2.2959 mL | 4.5919 mL | |
| 10 mM | 0.2296 mL | 1.1480 mL | 2.2959 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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