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TC-N 1752 is an orally active inhibitor of Nav1.7 channel with IC50 of 0.17 μM. TC-N 1752 shows analgesic activities.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $30 | In Stock | |
5 mg | $73 | In Stock | |
10 mg | $119 | In Stock | |
25 mg | $273 | In Stock | |
50 mg | $403 | In Stock | |
100 mg | $573 | In Stock | |
200 mg | $779 | In Stock | |
1 mL x 10 mM (in DMSO) | $80 | In Stock |
Description | TC-N 1752 is an orally active inhibitor of Nav1.7 channel with IC50 of 0.17 μM. TC-N 1752 shows analgesic activities. |
Targets&IC50 | Nav1.5 (human):1.1 μM (IC50), Nav1.3 (human):0.3 μM (IC50), Nav1.7 (human):0.17 μM (IC50), Nav1.4 (human):0.4 μM (IC50), Nav1.8 (human):0.1 μM (IC50) |
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[1]. 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)[1]. |
In vivo | TC-N 1752 (5 mg/ml; i.v.) attenuates Freund's adjuvant-induced sensitization of C fiber nociceptors[2]. 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[3]. |
Molecular Weight | 516.52 |
Formula | C25H27F3N6O3 |
Cas No. | 1211866-85-1 |
Smiles | CC(=O)Nc1cccc(Nc2ncnc(n2)N2CCC(CC2)OCc2ccc(OC(F)(F)F)cc2)c1C |
Relative Density. | 1.37 g/cm3 (Predicted) |
Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 112.5 mg/mL (217.8 mM), Sonication is recommended. 1eq. HCl: < 5.17 mg/mL | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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