Molecular Formula | C26H26N2O2
|
Molar Mass | 398.5 |
Density | 1.195±0.06 g/cm3(Predicted) |
Boling Point | 567.5±50.0 °C(Predicted) |
Solubility | DMSO : 160 mg/mL (401.51 mM; Need ultrasonic) |
pKa | 17.02±0.30(Predicted) |
Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
Use | TRPM8 antagonist 2 is an effective, selective TRPM8 antagonist with an IC50 value of 0.2 nM and can be used to study neuropathic pain syndrome. |
In vitro study | TRPM8 antagonist 2 (Compound 14) is a potent and selective TRPM8 antagonist, with an IC 50 of 0.2 nM, used in the research of neuropathic pain syndromes. TRPM8 antagonist 2 potently inhibits menthol-induced increase in intracellular Ca 2+ levels in Ca 2+ fluorimetric assays in HEK293 cells stably expressing the rat isoform of TRPM8 channels (IC 50 , 40 nM). |
In vivo study | TRPM8 antagonist 2 (1, 10, and 30 mg/kg, s.c.) shows a marked, dose-dependent antinociceptive activity, and inhibits wet-dog shakes (WDS)-like cold hypersensitivity in mice by 63% at 30 mg/kg. In addition, TRPM8 antagonist 2 (0.1 and 1 μg, s.c.) attenuates Oxaliplatin (OXP)-induced cold allodynia in mice. |