| Bioactivity | AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM[1]. |
| Invitro | AMG9678 potently inhibits the menthol and cold-induced increase in intracellular calcium in cells expressing rat TRPM8, the plasma half-life (T1/2) in rats is 7.6 h[1]. |
| In Vivo | AMG9678 (0-100 mg/kg; p.o.; once) produces a significant and somewhat dose-dependent decrease in body temperature (Tb) in rats[1].AMG9678 (30 mg/kg; p.o.; once daily for 4 consecutive days) decreases reduced body temperature after repeated dosing in rats[1]. Animal Model: |
| Name | AMG9678 |
| CAS | 1159997-27-9 |
| Formula | C20H18F6N2O |
| Molar Mass | 416.36 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Gavva NR, et al. Transient receptor potential melastatin 8 (TRPM8) channels are involved in body temperature regulation. Mol Pain. 2012 May 9;8:36. |