1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. TC-N 1752

TC-N 1752 

Cat. No.: HY-107405
Handling Instructions

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.

For research use only. We do not sell to patients.

TC-N 1752 Chemical Structure

TC-N 1752 Chemical Structure

CAS No. : 1211866-85-1

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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].

IC50 & Target[1][2]

hNav1.7

0.17 μM (IC50)

hNav1.8

0.1 μM (IC50)

hNav1.3

0.3 μM (IC50)

hNav1.4

0.4 μM (IC50)

hNav1.5

1.1 μM (IC50)

In Vitro

TC-N 1752 (compound 52) state-dependently inhibits Nav1.7, with IC50 of 170 nM on channels that are 20% inactivated and IC50 of 3.6 μM on fully noninactivated channels[1].
TC-N 1752 inhibits hNav1.7, hNav1.8, hNav1.9, rNav1.9, and mNav1.9 with IC50s of 0.2, 0.1, 1.6, 0.5 and 1.4 μM, respectively[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TC-N 1752 (compound 52) (3-30 mg/kg; p.o.) dose-dependently shows analgesic effect in the Formalin model[1].
TC-N 1752 (3-30 mg/kg; p.o.) decreases thermal hyperalgesia produced by inflammation[3].
TC-N 1752 (5 mg/mL; 500 μL; i.v.) attenuates complete Freund’s adjuvant (CFA)-induced sensitization of C-fiber nociceptors[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rats were injected intraplantar with Formalin[1]
Dosage: 3, 10, 20, 30 mg/kg
Administration: Administered p.o. 120 min prior to Formalin
Result: Showed analgesic efficacy starting at the dose of 3 mg/kg, with full efficacy at 20 mg/kg dose.
Molecular Weight

516.52

Formula

C₂₅H₂₇F₃N₆O₃

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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TC-N 1752
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