Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C15H27N5O5 |
Molecular Weight | 357.4054 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)C[C@H](NC(=O)[C@H]1O[C@@H]1C(O)=O)C(=O)NCCCCNC(N)=N
InChI
InChIKey=LTLYEAJONXGNFG-DCAQKATOSA-N
InChI=1S/C15H27N5O5/c1-8(2)7-9(20-13(22)10-11(25-10)14(23)24)12(21)18-5-3-4-6-19-15(16)17/h8-11H,3-7H2,1-2H3,(H,18,21)(H,20,22)(H,23,24)(H4,16,17,19)/t9-,10-,11-/m0/s1
Molecular Formula | C15H27N5O5 |
Molecular Weight | 357.4054 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/1440613
Sources: https://www.ncbi.nlm.nih.gov/pubmed/1440613
E-64 is an inhibitor of calpain and other cysteine proteases such as cathepsin B, cathepsin L, cathepsin H. The low toxic effects of the inhibitor, in addition to its effective mechanism of action, makes E-64 a potential template for drugs to treat diseases where high levels of a cysteine proteases are the primary cause. It was discovered, that this drug slowed the rate of formation of cataract in cultured rat lenses, but this study was discontinued.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4072 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7044372 |
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Target ID: CHEMBL3837 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7044372 |
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Target ID: CHEMBL2225 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7044372 |
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Target ID: CHEMBL3038466 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1848210 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2284926
in rats teratogenic effects: Wistar rats were injected with 10-30 mg/kg of E-64 intra-peritoneally on days 9 and 10 of gestation
Route of Administration:
Intraperitoneal
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19530614
Curator's Comment: The rapeutic effect of E-64, a broad spectrum cystine protease inhibitor against Giardia lamblia excystation was studied in vitro and in vivo. Giardia lamblia cysts incubated with E 64 in vitro completely failed in excystation in 90% while trophozoites released on 10% (partially excysted on 5% and completely excysted on 5%) compared to 90 % completely excysted on other non incubated (without E-64) of cysts beside, the trophozoites didn't release on 10% (partially excysted on 5% & completely non-excysted on 5%).
Unknown
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 18:10:19 GMT 2023
by
admin
on
Fri Dec 15 18:10:19 GMT 2023
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Record UNII |
R76F7856MV
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Record Status |
Validated (UNII)
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Record Version |
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E-64
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DTXSID90985271
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