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Submit ReviewTC-N 1752 is a 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.
TC-N 1752 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 51.65 | 100 | |
1eq. HCl | 5.17 | 10 |
The following data is based on the product molecular weight 516.52. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for TC-N 1752, please let us know.
Keywords: TC-N 1752, TC-N 1752 supplier, TCN1752, sodium, channels, blockers, selective, nav, analgesics, Voltage-gated, Sodium, Channels, 4435, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for TC-N 1752 include:
Curtright et al (2015) Modeling nociception in zebrafish: a way forward for unbiased analgesic discovery. PLoS One 10 e0116766 PMID: 25587718
Do you know of a great paper that uses TC-N 1752 from Tocris? Please let us know.
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Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.