MIV-247是选择性的组织蛋白酶S(cathepsinS)抑制剂，对人，小鼠和食蟹猴组织蛋白酶S的Ki值分别为2.1，4.2和7.5nM。
货号:ajcx12492
CAS:1352817-76-5
分子式:C17H24F3N3O4
分子量：391.39
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.

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].

[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.

Protocol:

Animal experiment:	Mice[1]MIV-247 is administered via oral gavage to Male C57BL/6 mice (20-30 g) at a dose volume of 5 ml/kg at doses up to 200 μmol/kg. In the PK studies, seven blood samples (20 μL) are drawn from the lateral saphenous vein of each mouse at 15 minutes, 30 minutes, 1 hour, 2 hours, 3 hours, 5 hours, and 7 hours postdose[1].
参考文献: [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.