2-Oxiranecarboxylicacid,3-[[[(1S)-3-methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]amino]carbonyl]-,(2S,3S)-
E-64c
CAS: 76684-89-4
Molecular Formula: C15H26N2O5
2-Oxiranecarboxylicacid,3-[[[(1S)-3-methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]amino]carbonyl]-,(2S,3S)- - Names and Identifiers
2-Oxiranecarboxylicacid,3-[[[(1S)-3-methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]amino]carbonyl]-,(2S,3S)- - Physico-chemical Properties
| Molecular Formula | C15H26N2O5 |
| Molar Mass | 314.38 |
| Appearance | White to off-white solid |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| MDL | MFCD00132882 |
| Use | Cysteine protease inhibitor; membrane-impermeable calpain inhibitor. Significantly reduces calpain-mediated depletion of microtubule-associated protein (MAP2) in an animal model of an ischemic brain. |
| In vitro study | E-64c, a derivative of a naturally occurring cysteine protease epoxide inhibitor, containing papain; Particularly with respect to hydrogen bonding and hydrophobic interactions of the ligand with conserved residues in the catalytic binding site [1]. E 64c(k2 / Ki = 140±5 M-1s-1) was shown to lead the development of irreversible Cathepsin C inhibitors. |
| In vivo study | E-64c/2 of plasma t-1 is 0.48 hours. There was no E-64c hemodynamic effect at this dose. The effect of reperfusion (p = 0.0016) or E-64c(p = 0.0226) per se on infarct size was significant using two-way ANOVA. When comparing Group A with Group B and Group C with Group D, E-64c of the treatment groups (groups A and C) consumption of CPK was slightly lower in the vehicle-injected groups (groups B and D). The lack of efficacy of E-64c alone can be explained by early dosing and a relatively short t-1/2. Since the effectiveness of NCO-700 has been established, our findings may suggest that E-64c has a small but beneficial effect on infarct size and CPK content. |
2-Oxiranecarboxylicacid,3-[[[(1S)-3-methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]amino]carbonyl]-,(2S,3S)- - Risk and Safety
| WGK Germany | 3 |
| RTECS | RR0404200 |
| HS Code | 29241990 |
2-Oxiranecarboxylicacid,3-[[[(1S)-3-methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]amino]carbonyl]-,(2S,3S)- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.181 ml | 15.904 ml | 31.809 ml |
| 5 mM | 0.636 ml | 3.181 ml | 6.362 ml |
| 10 mM | 0.318 ml | 1.59 ml | 3.181 ml |
| 5 mM | 0.064 ml | 0.318 ml | 0.636 ml |
Last Update：2024-01-02 23:10:35
2-Oxiranecarboxylicacid,3-[[[(1S)-3-methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]amino]carbonyl]-,(2S,3S)- - Reference Information
| Description | E 64c is a derivative of the natural epoxide inhibitor of cysteine protease (cysteine proteases), and is also a calcium ion activated neutral protease (CANP) Inhibitor and a weak irreversible inhibitor of cathepsin C (cathepsin C). |
| target | Cysteine proteases, CANP, Cathepsin C. TargetValue cysteine protease |
| In vitro study | E-64c, a naturally occurring derivative of cysteine protease epoxide inhibitor, containing papain; especially about ligand and catalytic binding site The hydrogen bond and hydrophobic interaction of conservative residues in the site [1]. E 64c(k2 / Ki = 140±5 M-1s-1) proved to be the lead structure for the development of irreversible cathepsin C inhibitors. |
| in vivo study | the t-1/2 of plasma E-64c is 0.48 hours. There is no E-64c hemodynamic effect at this dose. The effect of reperfusion (p = 0.0016) or E-64c(p = 0.0226) per se on infarct size was significant using two-way ANOVA. When comparing group A with group B and group C with group D, the consumption of CPK in the E-64c treatment group (group A and group C) was slightly lower than that in the group with the injection vehicle (group B and group D). The lack of effect of E-64c alone can be explained by early administration and relatively short t-1/2. Since the validity of the NCO-700 has been established, our results may indicate that E-64c has a small but beneficial effect on infarct size and CPK content. |
| animal experiment | dog study was conducted in 83 mongrel dogs with an average weight of 11.2kg. They were anesthetized with intravenous sodium thiourea (7mg/kg). E-64c dissolved in saturated sodium bicarbonate (100 mg/kg) was given by intravenous bolus (n = 17) before occlusion and immediately after reperfusion in group A, while group B (n = 17) received only carrier solution. At these times. In the remaining 49 dogs (group C and group D), LAD was permanently ligated at the same level and injected intravenously with Loxistatin acid (100mg/kg)(group C; n = 24) or only with the carrier (group D; group n = 25) before ligation and 1 hour after ligation. The E-64c dose is designed for its possible use in clinical practice. The estimated molecular concentration of loxetine acid in myocardium is 1,000 times the total amount of mCANP. |
| biological activity | Loxistatin Acid (E-64C, NSC 694279, EP 475), a E-64 derivative, is an irreversible membrane permeability cysteine protease inhibitor. Cysteine protease cathepsin L is required for SARS-CoV-2 virus invasion. |
| Target | Value |
Last Update：2024-04-10 22:29:15
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CAS: 76684-89-4
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CAS: 76684-89-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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