product name Loxistatin Acid (E-64C)
Description: Loxistatin Acid (also known as E-64C), an analog of E-64, is a potent, irreversible and membrane-permeable cysteine protease inhibitor. E-64-c has proved to be substantially more reactive than E-64 with cathepsins B and L. Cathepsins B and H from human liver and rat cathepsin L were used to measure the rate constants of inhibition of E-64-c, which indicated the rate constants of inactivation of cathepsins B, H and L were 298000, 2018, 206000 M-1 s-1 , respectively.
References: Biochem Biophys Res Commun. 1989 Jan 31;158(2):432-5; J Neurosci Res. 2003 Nov 1;74(3):393-405.
314.38
Formula
C15H26N2O5
CAS No.
76684-89-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 62 mg/mL (197.2 mM)
Water: 2 mg/mL (6.4 mM)
Ethanol: 62 mg/mL (197.2 mM)
Solubility (In vivo)
Saline: 2mg/mL
Synonyms
NSC 694279, EP 475
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19409616
| In Vitro |
In vitro activity: Loxistatin Acid (E-64C), as a thiol protease inhibitor, inhibits calpain activity in intact platelets. E-64C inhibits β-secretase activity in regulated secretory vesicles of neuronal chromaffin cells, and decrease Aβ production, indicating a therapeutic strategy for Alzheimers disease. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In pectoral muscle of dystrophic chickens, Loxistatin Acid (E-64C) normalizes the increased activities of cathepsin B and cathepsin H. E-64C inhibits ischemic degradation of cerebral proteins following occlusion of the middle cerebral artery in rats. |
| Animal model | Male Sprague-Dawley rats. |
| Formulation & Dosage | Dissolved in a small amount of saturated bicarbonate solution and then diluted with 0.9% NaCl saline; 400 mg/kg; i.p. injection |
| References | Biochem Biophys Res Commun. 1989 Jan 31;158(2):432-5; J Neurosci Res. 2003 Nov 1;74(3):393-405; J Biol Chem. 1991 Aug 5;266(22):14771-7. |
