TC-N 1752

TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain[1][2][3].

Product Specifications

CAS Number

[1211866-85-1]

UNSPSC

12352005

Target

Sodium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/tc-n-1752.html

Concentration

10mM

Purity

99.67

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

FC(F)(F)OC(C=C1)=CC=C1COC(CC2)CCN2C3=NC=NC(NC4=C(C(NC(C)=O)=CC=C4)C)=N3

Molecular Formula

C25H27F3N6O3

Molecular Weight

516.52

References & Citations

[1]Bregman H, et, al. Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain. J Med Chem. 2011 Jul 14;54 (13) :4427-45.|[2]Lin Z, et, al. Biophysical and Pharmacological Characterization of Nav1.9 Voltage Dependent Sodium Channels Stably Expressed in HEK-293 Cells. PLoS One. 2016 Aug 24;11 (8) :e0161450.|[3]Matson DJ, et, al. Inhibition of Inactive States of Tetrodotoxin-Sensitive Sodium Channels Reduces Spontaneous Firing of C-Fiber Nociceptors and Produces Analgesia in Formalin and Complete Freund's Adjuvant Models of Pain. PLoS One. 2015 Sep 17;10 (9) :e0138140.