TC-N 1752

TC-N 1752

• CAS Number: 1211866-85-1
• UNSPSC Description: 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].
• Target Antigen: 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
• 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 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.
• Shipping Conditions: Room Temperature
• Storage Conditions: -20°C, 3 years; 4°C, 2 years (Powder)
• Clinical Information: No Development Reported