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Nav1.8-IN-1
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Catalog No. T8579Cas No. 1026822-49-0
Alias CHEMBL1270208, 5-(4-Chlorophenyl)-N-[[2-(2,2,2-trifluoroethoxy)pyridin-3-yl]methyl]pyridine-3-carboxamide
Nav1.8-IN-1 (CHEMBL1270208) is an inhibitor of human NaV1.8
Nav1.8-IN-1
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Purity: 97.59%
Catalog No. T8579Alias CHEMBL1270208, 5-(4-Chlorophenyl)-N-[[2-(2,2,2-trifluoroethoxy)pyridin-3-yl]methyl]pyridine-3-carboxamideCas No. 1026822-49-0
Nav1.8-IN-1 (CHEMBL1270208) is an inhibitor of human NaV1.8
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $56 | In Stock | In Stock | |
| 5 mg | $125 | In Stock | In Stock | |
| 10 mg | $190 | In Stock | In Stock | |
| 25 mg | $313 | In Stock | In Stock | |
| 50 mg | $441 | In Stock | In Stock | |
| 100 mg | $596 | In Stock | In Stock | |
| 200 mg | $791 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $146 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:97.59%
Appearance:Solid
Color:White
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Product Introduction
Nav1.8-IN-1 AI Summary
Nav1.8-IN-1 exhibits various bioactivities and significant pharmacokinetic properties. It demonstrates high plasma protein binding (PPB = 99.87%) and has a brain-to-plasma ratio of 1.0, indicating comparable concentrations in both compartments. The compound has a moderate volume of distribution at steady state (Vdss = 2.0 L.kg-1) and plasma clearance of 10.0 mL.min-1.kg-1. Notably, it shows excellent oral bioavailability in rats (F = 95.0%) but limited aqueous solubility (3.1 µg.mL-1).
Pharmacologically, Nav1.8-IN-1 inhibits several ion channels and receptors, including hERG, human NaV1.5, NaV1.2, tetrodotoxin-resistant NaV1.8, and mouse NaV1.8, with varying IC50 values. It significantly inhibits chloride channels (>70.0% inhibition at 10 µM) and has demonstrated analgesic activity in a rat model of neuropathic pain (ED50 = 65.0 mg.kg-1, Emax = 66.0%). However, it shows minimal activity against TRPV1, P2X2/3 receptor, CaV2.2, and KCNQ2/Q3, with IC50 values exceeding 10,000 nM.
Regarding antiviral properties, Nav1.8-IN-1 exhibits SARS-CoV-2 3CL-Pro protease inhibition with a 12.41% inhibition rate at 20 µM. In high content imaging assays, the compound showed negligible inhibition (−0.04%) of VERO-6 cell cytotoxicity at 10 µM after 48 hours of exposure to the virus.
In various cell types, Nav1.8-IN-1 demonstrates cell-type-dependent effects on cell viability. It promotes consistent positive growth rates (0.81-0.84) in HEK293T cells, but has a mixed impact on U2OS and human fibroblast cells, with observed growth rates ranging from negative (-1.0) to positive (0.98).
Overall, Nav1.8-IN-1 is a pharmacologically diverse compound with substantial binding characteristics, variable pharmacokinetic properties, and distinct biological activities across different cell types and targets..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Nav1.8-IN-1 (CHEMBL1270208) is an inhibitor of human NaV1.8 |
| Synonyms | CHEMBL1270208, 5-(4-Chlorophenyl)-N-[[2-(2,2,2-trifluoroethoxy)pyridin-3-yl]methyl]pyridine-3-carboxamide |
| Molecular Weight | 421.8 |
| Formula | C20H15ClF3N3O2 |
| Cas No. | 1026822-49-0 |
| Smiles | C(NCC1=C(OCC(F)(F)F)N=CC=C1)(=O)C2=CC(=CN=C2)C3=CC=C(Cl)C=C3 |
| Relative Density. | 1.355 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 10 mg/mL (23.71 mM), Sonication is recommended.  | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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