Bioactivity | AMG8788 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 63.2 nM[1]. |
Invitro | AMG8788 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 6.7 h[1]. |
In Vivo | AMG8788 (30 mg/kg; p.o.; once) elicits a transient decrease in body temperature (Tb) in rats[1]. Animal Model: |
Name | AMG8788 |
CAS | 1159996-43-6 |
Formula | C23H18F4N2O |
Molar Mass | 414.40 |
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. |