Bioactivity | MIV-247 is a selective cathepsin S inhibitor with Kis of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively. |
In Vivo | Oral administration of MIV-247 (100-200 µmol/kg) dose-dependently attenuates mechanical allodynia by up to approximately 50% reversal when given as a single dose or when given twice daily for 5 days. Cathepsin S inhibition with MIV-247 exerts significant antiallodynic efficacy alone, and also enhances the effect of gabapentin and pregabalin without increasing side effects or inducing pharmacokinetic interactions[1]. |
Name | MIV-247 |
CAS | 1352817-76-5 |
Formula | C17H24F3N3O4 |
Molar Mass | 391.39 |
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]. Hewitt E. et al. Selective Cathepsin S Inhibition with MIV-247 Attenuates Mechanical Allodynia and Enhances the Antiallodynic Effects of Gabapentin and Pregabalin in a Mouse Model of Neuropathic Pain. J Pharmacol Exp Ther. 2016 Sep;358(3):387-96. |