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 | |
| Cell Lines | Osteoclasts | |
| Concentrations | 5 μM | |
| 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. |
| Molecular Weight | 357.41 |
| Formula | C15H27N5O5 |
| CAS Number | 66701-25-5 |
| Solubility (25°C) | DMSO 57 mg/mL Water 5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
[2] Gregory Blass, et al. Chronic cathepsin inhibition by E-64 in Dahl salt-sensitive rats
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