| Description |
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.
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| Related Catalog |
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| Target |
IC50: 2.1 nM (Human Cathepsin S), 4.2 nM (Mouse Cathepsin S), 7.5 nM (Cynomolgus monkey Cathepsin S)[1]
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| 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].
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| Animal Admin |
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].
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| 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.
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