1. Metabolic Enzyme/Protease
  2. Proteasome
    Cathepsin

E 64c 

Cat. No.: HY-100227
Handling Instructions

E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor.

For research use only. We do not sell to patients.

E 64c Chemical Structure

E 64c Chemical Structure

CAS No. : 76684-89-4

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor.

IC50 & Target

Cysteine proteases[1], CANP[2], Cathepsin C[3].

In Vitro

E-64c, a derivative of naturally occurring epoxide inhibitor of cysteine proteases, with papain; especially with regard to the hydrogen bonding and hydrophobic interactions of the ligands with conserved residues in the catalytic binding site[1]. E 64c (k2/Ki=140±5M-1s-1) is demonstrated to be a lead structure for the development of irreversible cathepsin C inhibitors[3].

In Vivo

The t-1/2 of plasma E-64c is 0.48 hours. The hemodynamic effects of E-64c are absent at this dose. Using two way analysis of variance, the effects of reperfusion (p=0.0016) or E-64c (p=0.0226) per se on infarct size are significant. In comparing Group A with Group B and Group C with Group D, the depletion of CPK in the E-64c treated groups (Groups A and C) is slightly less than in the vehicle-injected groups (Groups B and D). The insufficient effect of E-64c alone may be explained by the early administration and relatively short t-1/2. Since the effectiveness of NCO-700 has been established,6),7) our findings might indicate a small but beneficial effect of E-64c on infarct size and CPK content[2].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1809 mL 15.9043 mL 31.8086 mL
5 mM 0.6362 mL 3.1809 mL 6.3617 mL
10 mM 0.3181 mL 1.5904 mL 3.1809 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2]

Dogs[2]
Studies are carried out in 83 mongrel dogs with a mean weight of 11.2kg. They are anesthetized with intravenous sodium thiamylal (7mg/kg). An intravenous bolus of E-64c (100mg/kg), dissolved in saturated sodium bicarbonate, is administered immediately before the occlusion and after reperfusion in Group A (n=17), whereas Group B (n=17) receive only the vehicle solution at these times. In the remaining 49 dogs (Groups C and D), the LAD is permanently ligated at the same level and an intravenous bolus of either Loxistatin acid (100mg/kg) (Group C; n=24) or vehicle only (Group D; n=25) is given immediately before and 1 hour after the ligation. The dose of E-64c is designed for its possible use in clinical practice and the estimated intramyocardial Loxistatin acid molecular concentration is 1,000 times that of total mCANP[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

314.38

Formula

C₁₅H₂₆N₂O₅

CAS No.

76684-89-4

SMILES

O=C([[email protected]]1O[[email protected]@H]1C(N[[email protected]](C(NCCC(C)C)=O)CC(C)C)=O)O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
E 64c
Cat. No.:
HY-100227
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E 64c

Cat. No.: HY-100227