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E-64

Cat. No. M2659
E-64 Structure
Size Price Availability Quantity
5mg USD 46  USD46 In stock
10mg USD 72  USD72 In stock
25mg USD 140  USD140 In stock
50mg USD 250  USD250 In stock
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Quality Control & Documentation
Biological Activity

E-64 is an irreversible and selective cysteine protease inhibitor with IC50 of 9 nM for papain.

Customer Product Validations & Biological Datas
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.
Chemical Information
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
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] Bangzuo Liu, et al. Small molecule inhibitor E-64 exhibiting the activity against African swine fever virus pS273R

[2] Gregory Blass, et al. Chronic cathepsin inhibition by E-64 in Dahl salt-sensitive rats

[3] Zifeng Zhang, et al. Therapeutic Efficacy of E-64-d, a Selective Calpain Inhibitor, in Experimental Acute Spinal Cord Injury

[4] Mohit Wadhawan, et al. Inhibition of cathepsin B by E-64 induces oxidative stress and apoptosis in filarial parasite

[5] No authors listed. Drugs R D. E 64

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