[CAS NO. 1211866-85-1] TC-N 1752
PRODUCTS SPECIFICATIONS [1211866-85-1]
DESCRIPTION [1211866-85-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 516.52 |
| Molecular Formula | C25H27F3N6O3 |
| SMILES | FC(F)(F)OC(C=C1)=CC=C1COC(CC2)CCN2C3=NC=NC(NC4=C(C(NC(C)=O)=CC=C4)C)=N3 |
Summary
TC-N 1752 is a potent and orally active inhibitor of Nav1.7 , with IC 50 s 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
|
hNa v 1.7 0.17 μM (IC 50 ) |
hNa v 1.8 0.1 μM (IC 50 ) |
hNa v 1.3 0.3 μM (IC 50 ) |
hNa v 1.4 0.4 μM (IC 50 ) |
hNa v 1.5 1.1 μM (IC 50 ) |
In Vitro
TC-N 1752 (compound 52) state-dependently inhibits Nav1.7, with IC
50
of 170 nM on channels that are 20% inactivated and IC
50
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 IC
50
s 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 242.00 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9360 mL | 9.6802 mL | 19.3603 mL |
| 5 mM | 0.3872 mL | 1.9360 mL | 3.8721 mL |
| 10 mM | 0.1936 mL | 0.9680 mL | 1.9360 mL |
References
- [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):e013