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.
Compound Libraries
TC-N 1752 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 516.52 |
| Formula | C25H27F3N6O3 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1211866-85-1 |
| PubChem ID | 53361524 |
| InChI Key | QLKAFHZJICDACE-UHFFFAOYSA-N |
| Smiles | CC(C(NC(C)=O)=CC=C4)=C4NC1=NC=NC(N2CCC(OCC3=CC=C(OC(F)(F)F)C=C3)CC2)=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
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
References
References are publications that support the products' biological activity.
Bregman et 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
Lin et al (2016) Biophysical and pharmacological characterization of Nav1.9 voltage dependent sodium channels stably expressed in HEK-293 cells. PLoS One. 11 PMID: 27556810
Keywords: TC-N 1752, supplier, TCN1752, sodium, channels, blockers, selective, nav, analgesics, Voltage-gated, Sodium, Channels, Voltage-gated, Sodium, Channels, Tocris Bioscience
