MIV-247 |
رقم الكتالوجGC31106 |
MIV-247 هو مثبط انتقائي لكاثيبسين S مع Kis من 2.1 و 4.2 و 7.5 نانومتر للإنسان والفأر و cynomolgus monkey cathepsin S ، على التوالي
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Cas No.: 1352817-76-5
Sample solution is provided at 25 µL, 10mM.
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.
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