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Calpeptin

Name: Calpeptin
Brand: Selleck Chemicals
SKU: S7396
Rating: 5 (26 reviews)

Catalog No.S7396 Purity:97%

Calpeptin is a potent, cell-permeable calpain inhibitor with ID50 of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets), respectively. Calpeptin attenuates apoptosis and intracellular inflammatory changes in muscle cells.

Calpeptin Chemical Structure

CAS No. 117591-20-5

Purity & Quality Control

Batch: Purity: >97%

Calpeptin Related Products

Related Targets	Cathepsin Calpain Cruzain Papainb Cathepsin	Click to Expand
Related Products	Aloxistatin (E64d) Odanacatib MG-101 (ALLN) E-64 Z-FA-FMK NEM (N-Ethylmaleimide) Cathepsin Inhibitor 1 PD 151746 Loxistatin Acid (E-64C)	Click to Expand
Related Compound Libraries	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Protease Inhibitor Library Ubiquitination Compound Library	Click to Expand

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
PC12	Autophagy assay	10 uM	96 hrs	Induction of autophagy in undifferentiated rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as EGFP-HDQ74 clearance at 10 uM after 96 hrs by calpain activation assay	18391949
PC12	Autophagy assay	10 uM	96 hrs	Induction of autophagy in differentiated rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 10 uM after 96 hrs by calpain activation assay	18391949
COS7	Autophagy assay	50 uM	48 hrs	Induction of autophagy in african green monkey COS7 cells expressing EGFP-HDQ74 assessed as inhibition of PLC-epsilon overexpression-induced EGFP-HDQ74 aggregation at 50 uM after 48 hrs	18391949
PC12	Autophagy assay	10 uM	96 hrs	Induction of autophagy in undifferentiated rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 10 uM after 96 hrs by calpain activation assay	18391949
PC12	Autophagy assay	10 uM	96 hrs	Induction of autophagy in differentiated rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as EGFP-HDQ74 clearance at 10 uM after 96 hrs by calpain activation assay	18391949
HeLa	Autophagy assay	50 uM		Induction of autophagy in human HeLa cells expressing EGFP-LC3 assessed as increase in LC3-2 level at 50 uM in presence of 400 nM bafilomycin A1	18391949
COS7	Autophagy assay	50 uM	24 hrs	Induction of autophagy in african green monkey COS7 cells assessed as increase in autophagosome at 50 uM after 24 hrs by electron microscopy	18391949
COS7	Autophagy assay	50 uM	48 hrs	Induction of autophagy in african green monkey COS7 cells expressing EGFP-HDQ74/rheb assessed as reduction in EGFP-HDQ74 aggregation at 50 uM after 48 hrs	18391949
COS7	Autophagy assay	50 uM	24 hrs	Induction of autophagy in african green monkey COS7 cells expressing EGFP-LC3 assessed as increase in EGFP-LC3 vesicle at 50 uM after 24 hrs	18391949
HeLa	Antiviral assay			Antiviral activity against human rhinovirus-14 in HeLa cells, IC50=17.7μM.	ChEMBL
HeLa	Cytotoxic assay			Cytotoxic activity against HeLa cells using XTT assay, TC50=22.1μM.	ChEMBL
NMuMG	Function assay	25 to 50 uM	24 to 72 hrs	Inhibition of calpain in mouse NMuMG cells assessed as suppression of TGFbeta1-induced calpain activity by measuring Filamin-A levels at 25 to 50 uM incubated for 24 to 72 hrs by Western blot analysis	ChEMBL
NMuMG	Function assay	25 to 50 uM	24 to 72 hrs	Inhibition of calpain in mouse NMuMG cells assessed as suppression of TGFbeta1-induced EMT by measuring alpha-SMA expression at 25 to 50 uM incubated for 24 to 72 hrs by Western blot analysis	ChEMBL
Click to View More Cell Line Experimental Data

Biological Activity

Description

Targets

Calpain II (porcine kidney) ^[1]	Calpain I (human platelets) ^[1]	Calpain I (porcine erythrocytes) ^[1]	Papainb ^[1]
34 nM(ID50)	40 nM(ID50)	52 nM(ID50)	138 nM(ID50)

In vitro
In vitro	Calpeptin inhibits 20K phosphorylation in a dose-related manner in platelets stimulated by thrombin, ionomycin or collagen. ^[1] In differentiating PC12 cells, Calpeptin promotes neurite elongation via inhibition of Calpain activity. ^[2] In rat retinal ganglion cells, Calpeptin attenuates apoptosis, maintains normal whole-cell membrane potential, and thus provides functional neuroprotection. ^[3]
Experimental Result Images	Methods	Biomarkers	Images	PMID
Experimental Result Images	Immunofluorescence	Src / EGFR		29641465

In Vivo
In vivo	In a feline right ventricular (RV) PO (RVPO) model, calpeptin (0.6 mg/kg, i.v.) blocks the activation of calpain and caspase-3, cleavage of their substrates, and cardiomyocyte programmed cell death. ^[4] In a rat focal cerebral ischemia–reperfusion injury model, Calpeptin reduces the neuronal apoptosis in hippocampal CA1 sector via inhibition of the expression of Caspase-3. ^[5]
Animal Research	Animal Models	Feline right ventricular (RV) PO (RVPO) model
	Dosages	0.6 mg/kg
	Administration	i.v.

References

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Chemical Information & Solubility

Molecular Weight	362.46	Formula	C₂₀H₃₀N₂O₄
CAS No.	117591-20-5	SDF	Download Calpeptin SDF
Smiles	CCCCC(C=O)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 72 mg/mL ( (198.64 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 72 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.600mg/ml (9.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 72 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.600mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

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Calculation results:

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.

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

Tel: +1-832-582-8158 Ext:3
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