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MIV-247

Catalog No. T12051   CAS 1352817-76-5

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.

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MIV-247 Chemical Structure
MIV-247, CAS 1352817-76-5
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Purity: 99.31%
ee: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Targets&IC50 Cathepsin S (cynomolgus monkey):7.5 nM, Cathepsin S (mouse):4.2 nM, Cathepsin S (human):2.1 nM
In vivo To assess the potential neurobehavioral side effects of MIV-247, oral administration of MIV-247 (100-200 μmol/kg) resulted in a dose-dependent reduction of mechanical allodynia, with up to approximately 50% reversal observed after single or twice-daily dosing for 5 days. No behavioral deficits were observed with any dose of MIV-247 tested[1].
Molecular Weight 391.39
Formula C17H24F3N3O4
CAS No. 1352817-76-5

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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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Keywords

MIV-247 1352817-76-5 Proteases/Proteasome Cysteine Protease MIV 247 MIV247 inhibitor inhibit

 

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