| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
Sodium Channel inhibitor 1 targets voltage-gated sodium (Nav) channels, specifically the Nav1.7 subtype with an IC₅0 of 0.16 microM. Nav1.7 is a voltage-gated sodium channel that plays a critical role in pain signaling and is expressed primarily in peripheral sensory neurons and sympathetic ganglia. Gain-of-function mutations in Nav1.7 are associated with inherited pain disorders, while loss-of-function mutations cause congenital insensitivity to pain. By blocking Nav1.7, Sodium Channel inhibitor 1 inhibits sodium ion influx, reducing neuronal excitability and pain signal transmission. The compound represents a novel type of selective voltage-gated sodium channel blocker for pain treatment.
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| ln Vitro |
In vitro, Sodium Channel inhibitor 1 blocks voltage-gated sodium channels with an IC₅0 of 0.16 microM for Nav1.7. The compound is a novel and selective voltage-gated sodium channel blocker that may be utilized in pain research. In cellular assays using cells expressing Nav1.7 channels, the compound inhibits sodium currents in a concentration-dependent manner. Electrophysiological studies (patch-clamp) demonstrate that the compound blocks sodium channel conductance, reducing action potential firing in sensory neurons. The compound's selectivity for Nav1.7 over other sodium channel subtypes and its potency support its use as a tool for studying pain mechanisms.
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| ln Vivo |
In vivo, Sodium Channel inhibitor 1 demonstrates concentration-dependent efficacy in preclinical behavioral pain models. The compound's ability to block Nav1.7 channels makes it a potential candidate for pain treatment. In animal models of pain (e.g., formalin test, CFA-induced inflammatory pain, neuropathic pain models), the compound may reduce pain behaviors such as paw withdrawal, licking, and flinching. However, specific in vivo efficacy data, dosing regimens, and pharmacokinetic profiles are limited in publicly available sources. The compound is a research-grade small molecule and is not a clinically approved drug.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Sodium Channel inhibitor 1 involve measuring binding affinity and functional activity at voltage-gated sodium channels. Radioligand binding assays using [3H]-saxitoxin or [3H]-tetrodotoxin (TTX) can be performed using membrane preparations from cells expressing Nav1.7 channels. Membranes are incubated with varying concentrations of the compound in assay buffer at room temperature for 60-90 minutes. Bound and free radioligands are separated by rapid filtration. Filter-bound radioactivity is quantified by liquid scintillation counting. IC₅0 values for inhibition of radioligand binding are determined from dose-response curves.
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| Cell Assay |
Cellular assays for Sodium Channel inhibitor 1 are performed using cells expressing voltage-gated sodium channels, such as HEK-293 or CHO cells transfected with Nav1.7. Whole-cell patch-clamp electrophysiology is used to measure sodium currents. Cells are voltage-clamped at -80 mV and step-depolarized to test potentials to activate sodium channels. Varying concentrations of the compound (0.001-10 microM) are applied, and inhibition of peak sodium current is measured. IC₅0 values for channel blockade are calculated from dose-response curves. For high-throughput screening, fluorescence-based membrane potential assays or calcium influx assays can be used. Selectivity is assessed against other Nav subtypes (Nav1.1, Nav1.2, Nav1.5, Nav1.8).
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| Animal Protocol |
In vivo animal studies for Sodium Channel inhibitor 1 are conducted in rodent models of pain. In typical protocols, mice or rats are administered the compound orally, intraperitoneally, or subcutaneously at doses of 1-30 mg/kg. Pain models include the formalin test (acute inflammatory pain), carrageenan-induced paw edema (inflammatory pain), chronic constriction injury (neuropathic pain), and spinal nerve ligation (neuropathic pain). Pain behaviors (paw withdrawal threshold, paw withdrawal latency, licking, flinching) are measured. Pharmacokinetic parameters are determined from plasma and brain samples by LC-MS/MS. Efficacy is compared to vehicle control and standard analgesics (e.g., gabapentin, pregabalin).
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| ADME/Pharmacokinetics |
Sodium Channel inhibitor 1 (CAS#: 1198117-23-5) has molecular formula C24H1₉F4N3O3 and molecular weight 473.42. The compound is a novel and selective voltage-gated sodium channel blocker, specifically targeting Nav1.7 with an IC₅0 of 0.16 microM. It is a 3-oxoisoindoline-1-carboxamide derivative used in pain research. The compound is a research-grade small molecule and is not a clinically approved drug. Storage: powder at -20degC for up to 3 years; in solvent at -80degC for 1 year. The compound is soluble in DMSO. For research use only.
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| References | |
| Additional Infomation |
Sodium Channel inhibitor 1 (CAS#: 1198117-23-5) is a novel and selective voltage-gated sodium channel blocker, specifically targeting Nav1.7 with an IC₅0 of 0.16 microM. Nav1.7 is a voltage-gated sodium channel that plays a critical role in pain signaling and is expressed primarily in peripheral sensory neurons. Gain-of-function mutations in Nav1.7 are associated with inherited pain disorders, making it a key target for pain therapeutics. Sodium Channel inhibitor 1 demonstrates concentration-dependent efficacy in preclinical behavioral pain models. The compound is used in research to study sodium channel function and pain mechanisms. As of the current date, Sodium Channel inhibitor 1 is not approved for clinical use.
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| Molecular Formula |
C24H19F4N3O3
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|---|---|
| Molecular Weight |
473.4196
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| Exact Mass |
473.136
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| CAS # |
1198117-23-5
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| PubChem CID |
44545403
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| Appearance |
White to off-white solid powder
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| LogP |
4.953
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
714
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=NC(=C1)CCN2C(C3=C(C2=O)C=CC=C3F)C(=O)NCC4=CC=C(C=C4)OC(F)(F)F
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| InChi Key |
GRXUKFHZQDPFAI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H19F4N3O3/c25-19-6-3-5-18-20(19)21(31(23(18)33)13-11-16-4-1-2-12-29-16)22(32)30-14-15-7-9-17(10-8-15)34-24(26,27)28/h1-10,12,21H,11,13-14H2,(H,30,32)
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| Chemical Name |
7-fluoro-3-oxo-2-(2-pyridin-2-ylethyl)-N-[[4-(trifluoromethoxy)phenyl]methyl]-1H-isoindole-1-carboxamide
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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 (~211.23 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.28 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 | 2.1123 mL | 10.5614 mL | 21.1229 mL | |
| 5 mM | 0.4225 mL | 2.1123 mL | 4.2246 mL | |
| 10 mM | 0.2112 mL | 1.0561 mL | 2.1123 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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