Loxistatin Acid (E-64C)

Catalog No.S7392

Loxistatin Acid (E-64C), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor.

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Loxistatin Acid (E-64C) Chemical Structure

Loxistatin Acid (E-64C) Chemical Structure
Molecular Weight: 314.38

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description Loxistatin Acid (E-64C), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor.
Targets cysteine protease [1]
In vitro Loxistatin Acid (E-64C), as a thiol protease inhibitor, inhibits calpain activity in intact platelets. [1]E-64C inhibits β-secretase activity in regulated secretory vesicles of neuronal chromaffin cells, and decrease Aβ production, indicating a therapeutic strategy for Alzheimer's disease. [4]
In vivo In pectoral muscle of dystrophic chickens, Loxistatin Acid (E-64C) normalizes the increased activities of cathepsin B and cathepsin H. [2] E-64C inhibits ischemic degradation of cerebral proteins following occlusion of the middle cerebral artery in rats. [3]
Features

Protocol(Only for Reference)

Animal Study: [3]

Animal Models Male Sprague-Dawley rats.
Formulation Dissolved in a small amount of saturated bicarbonate solution and then diluted with 0.9% NaCl saline.
Dosages ~400 mg/kg
Administration i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] McGowan EB, et al. Biochem Biophys Res Commun. 1989, 158(2), 432-435.

[2] Noda T, et al. J Biochem. 1981, 90(3), 893-896.

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Chemical Information

Download Loxistatin Acid (E-64C) SDF
Molecular Weight (MW) 314.38
Formula

C15H26 N2 O5

CAS No. 76684-89-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms NSC 694279, EP 475
Solubility (25°C) * In vitro DMSO 62 mg/mL (197.21 mM)
Ethanol 62 mg/mL (197.21 mM)
Water 2 mg/mL (6.36 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-Oxiranecarboxylicacid,3-[[[(1S)-3-methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]amino]carbonyl]-,(2S,3S)-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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