Chemical Name:N-[2-Methyl-3-[[4-[4-[[4-(trifluoromethoxy)phenyl]methoxy]-1-piperidinyl]-1,3,5-triazin-2-yl]amino]phenyl]acetamide
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Human NaV channel inhibitor (IC50 values are 0.17, 0.3, 0.4, 1.1 and 1.6 μM at hNaV1.7, hNaV1.3, hNaV1.4, hNaV1.5 and hNav1.9 respectively). Also inhibits tetrodotoxin-sensitive sodium channels. Displays analgesic efficacy in the formalin pain model.
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Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
1eq. HCl
5.17
10
DMSO
51.65
100
ethanol
2.58
5
Preparing Stock Solutions
The following data is based on the product molecular weight 516.52. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
1.94 mL
9.68 mL
19.36 mL
5 mM
0.39 mL
1.94 mL
3.87 mL
10 mM
0.19 mL
0.97 mL
1.94 mL
50 mM
0.04 mL
0.19 mL
0.39 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Bregmanet al (2011) Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain. J.Med.Chem. 54 4427 PMID: 21634377
Linet al (2016) Biophysical and pharmacological characterization of Nav1.9 voltage dependent sodium channels stably expressed in HEK-293 cells. PLoS One. 11 PMID: 27556810