E-64 is an irreversible and selective cysteine protease inhibitor with IC50 of 9 nM for papain.
|Source||Arthritis Res Ther (2018). Figure 2. E-64|
|Method||Cell viability assay|
|Incubation Time||24 h|
|Results||In this study, the resorption of cortical bone in the presence of resorption inhibitors—the cysteine protease inhibitor E-64, the MMP inhibitor GM6001, and the VATPase inhibitor diphyllin—serve mainly as validation of functional resorption on the cortical bone slices and as a reference for the subchondral bone resorption in osteochondral ECM.|
|Solubility (25°C)||DMSO 57 mg/mL
Water 5 mg/mL
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 Bangzuo Liu, et al. Small molecule inhibitor E-64 exhibiting the activity against African swine fever virus pS273R
 Gregory Blass, et al. Chronic cathepsin inhibition by E-64 in Dahl salt-sensitive rats
 Zifeng Zhang, et al. Therapeutic Efficacy of E-64-d, a Selective Calpain Inhibitor, in Experimental Acute Spinal Cord Injury
 Mohit Wadhawan, et al. Inhibition of cathepsin B by E-64 induces oxidative stress and apoptosis in filarial parasite
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