Aloxistatin (E64d)

Catalog No.S7393 Synonyms: E-64d

For research use only.

Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry, and aloxistatin treatment reduced cellular entry of SARS-CoV-2 pseudovirions by 92.3%.

Aloxistatin (E64d) Chemical Structure

CAS No. 88321-09-9

Selleck's Aloxistatin (E64d) has been cited by 22 publications

Purity & Quality Control

Choose Selective Cysteine Protease Inhibitors

Biological Activity

Description Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry, and aloxistatin treatment reduced cellular entry of SARS-CoV-2 pseudovirions by 92.3%.
Targets
Cysteine protease [1]
In vitro

Aloxistatin can enter the intact platelet and inhibit proteolysis by inhibiting calpain. [2] Aloxistatin blunts Parathyroid hormone (PTH)-induced cell proliferation and inhibits differentiation osteoblasts in vitro. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U937 cells NV7lNZF[TnWwY4Tpc44h[XO|YYm= MXfCcI9kc2GmZTDv[kBk[XSqZYDzbY4hTyCycn;j[ZN{cW6pIHnuJIh2dWGwIGW5N|ch[2WubIOgZpkh\GWwc3n0c41mfHK7LDDJR|UxRTFwMTFOwG0> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV|NUiwNkc,OTd3M{W4NFI9N2F-
Assay
Methods Test Index PMID
Western blot LAMP-1 / Rab5 / pro-Ctsl / Ctsl / Ctsb / pro-Ctsd 25744631
Immunofluorescence LAMP-1 25744631
In vivo Aloxistatin (100 mg/kg, p.o.) strongly inhibits the cathepsin B&L activities in the skeletal muscle, heart and liver of hamsters. [1] In spinal cord injury (SCI) rats, Aloxistatin provides neuroprotection in SCI lesion and penumbra. [4] Aloxistatin reduces brain amyloid-β and improves memory deficits in Alzheimer's disease animal models by inhibiting cathepsin B activity. [5]

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: Hamsters
  • Dosages: ~100 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

DMSO 68 mg/mL
(198.58 mM)
Water Insoluble
Ethanol '68 mg/mL

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+corn oil
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 342.43
Formula

C17H30N2O5

CAS No. 88321-09-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC(=O)C1C(O1)C(=O)NC(CC(C)C)C(=O)NCCC(C)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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.

Handling Instructions

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