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MIV-247 

Cat. No. M28225
MIV-247  Structure
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Biological Activity

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.

Chemical Information
Molecular Weight 391.39
Formula C17H24F3N3O4
CAS Number 1352817-76-5
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ke Peng, et al. J Cell Physiol. Inhibition of cathepsin S attenuates myocardial ischemia/reperfusion injury by suppressing inflammation and apoptosis

[2] Ellen Hewitt, et al. J Pharmacol Exp Ther. 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

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  Catalog
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Keywords: MIV-247  supplier, Cathepsin, inhibitors, activators


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