| Description | MIV-247 is a selective and potent inhibitor of cathepsin S (Kis 2.1, 4.2, and 7.5 nM for human, mouse, and wild monkey cathepsin S, respectively), which attenuates mechanical anomalies in preclinical models of neuropathic pain, and can be used to study cardiac muscle injury. |
| In vivo | 为了评估 MIV-247 对神经行为的副作用。口服 MIV-247 （100-200 μmol/kg） 剂量依赖性减弱机械异常性疼痛，单次给药或每天两次给药，持续 5 天，最多约 50% 逆转，在测试的任何剂量的 MIV-247 中均未观察到行为缺陷[1]。 |
| Target activity | Cathepsin S (cynomolgus monkey):7.5 nM, Cathepsin S (mouse):4.2 nM, Cathepsin S (human):2.1 nM |
| molecular weight | 391.39 |
| Molecular formula | C17H24F3N3O4 |
| CAS | 1352817-76-5 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 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. |