TC-N 1752

SKU: orb1703993

Description

TC-N 1752 is a potent, orally bioavailable small molecule inhibitor of the voltage-gated sodium channel Nav1.7 (IC₅₀ = 0.17 µM). It demonstrates analgesic efficacy in preclinical models, making it a valuable research tool for investigating neuropathic pain mechanisms in both in vitro and in vivo studies.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1211866-85-1
• MW: 516.52
• Purity: 99.71% (May vary between batches)
• Formula: C₂₅H₂₇F₃N₆O₃
• SMILES: CC(=O)Nc1cccc(Nc2ncnc(n2)N2CCC(CC2)OCc2ccc(OC(F)(F)F)cc2)c1C
• Target: Sodium Channel
• Solubility: DMSO:112.5 mg/mL (217.8 mM)

Bioactivity

• Target IC50:
  Nav1.4 (human):0.4 μM (IC50)|Nav1.7 (human):0.17 μM (IC50)|Nav1.5 (human):1.1 μM (IC50)|Nav1.3 (human):0.3 μM (IC50)|Nav1.8 (human):0.1 μM (IC50)
• In Vivo:
  TC-N 1752 (5 mg/ml; i.v.) attenuates Freund's adjuvant-induced sensitization of C fiber nociceptors. TC-N 1752 (3-30 mg/kg; orally) exhibits analgesic effects in a dose-dependent manner in a formalin model and reduces thermal hyperalgesia produced by inflammation.
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• In Vitro:
  TC-N 1752 exhibits IC50s of 0.2, 0.1, 1.6, 0.5 and 1.4 μM for hNav1.7, hNav1.8, hNav1.9, rNav1.9, and mNav1.9. TC-N 1752 state-dependently inhibits Nav1.7 channel on channels that are 20% inactivated(IC50 = 170 nM) and on fully noninactivated channels(IC50 = 3.6 μM).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Nav1.7 channel, SodiumChannel, Sodium Channel, TC N 1752, TCN 1752, TC-N 1752, TC-N1752, TC-N-1752

Compound Identifiers

PubChem CID

53361524