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Chemical Structure| 117591-20-5 Chemical Structure| 117591-20-5

Structure of Calpeptin
CAS No.: 117591-20-5

Chemical Structure| 117591-20-5

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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.

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Product Details of Calpeptin

CAS No. :117591-20-5
Formula : C20H30N2O4
M.W : 362.46
SMILES Code : O=C(OCC1=CC=CC=C1)N[C@H](C(N[C@H](C=O)CCCC)=O)CC(C)C
MDL No. :MFCD00155623
InChI Key :PGGUOGKHUUUWAF-ROUUACIJSA-N
Pubchem ID :73364

Safety of Calpeptin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • Cysteine Protease

    Calpain I (porcine erythrocytes), ID50:52 nM

    Calpain II (porcine kidney), ID50:40 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Vero E6 cells 50 µM 12 hours to 24 hours To study the effect of Calpeptin on the cleavage of SARS-CoV-2 viral proteins, it was found that Calpeptin treatment significantly reduced the cleavage products at N19, S260, and S637 sites. PMC8455558
N2a cells 40 µM 24 hours To test the effect of Calpeptin on NF protein degradation in N2a cells, results showed that Calpeptin significantly increased the levels of all three NF proteins. PMC10012948
Rat primary cortical neurons 50 µM 24 hours To investigate the effect of Calpeptin on okadaic acid-induced cleavage of DLP1 and spectrin. Results showed that Calpeptin completely inhibited the okadaic acid-induced cleavage of DLP1 and spectrin. PMC6516178
HEK293 cells 30 µg/ml 3 hours To study the effect of Calpeptin on ABCA1 protein levels, results showed that Calpeptin treatment significantly increased ABCA1 protein levels. PMC151839
Mouse peritoneal macrophages 20 µg/ml 3 hours To study the effect of Calpeptin on ABCA1 protein levels in mouse peritoneal macrophages, results showed that Calpeptin treatment significantly increased ABCA1 protein levels. PMC151839
Mouse primary hepatocytes 15 µg/ml 3 hours To study the effect of Calpeptin on ABCA1 protein levels in mouse primary hepatocytes, results showed that Calpeptin treatment significantly increased ABCA1 protein levels. PMC151839
Bovine aortic endothelial cells 10 μM 30 minutes To investigate the effect of Calpeptin on VEGF-induced NO? production in endothelial cells, results showed that Calpeptin significantly inhibited VEGF-induced NO? production. PMC2720268
intestinal epithelial cells (IECs) 1 μg/ml 4 hours To study the effect of Calpeptin on caspase 3 activation in MDP-stimulated IECs, results showed that Calpeptin treatment prevented caspase 3 activation. PMC4362239
Rat hippocampal neurons 50 μM 4 hours To investigate the effect of Calpeptin on AMPA-induced down-regulation of TARPγ8 and GluA1 protein levels, results showed that Calpeptin significantly blocked the AMPA-induced down-regulation of TARPγ8 and GluA1. PMC4775841
Rat primary cortical neurons 50 µM 4 hours To investigate the effect of Calpeptin on glutamate-induced cleavage of DLP1 and spectrin. Results showed that Calpeptin significantly inhibited the glutamate-induced cleavage of DLP1 and spectrin. PMC6516178
Primary cortical neurons from CRND8 APP transgenic mice 50 µM 4 hours To investigate the effect of Calpeptin on DLP1 and spectrin cleavage in primary cortical neurons from CRND8 APP transgenic mice. Results showed that Calpeptin inhibited the cleavage of DLP1 and spectrin in CRND8 mouse neurons. PMC6516178

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Zebrafish Transgenic GFP-Lc3 zebrafish embryos Embryo water 50 μM 24 hours Calpeptin significantly induced the formation of Lc3-positive puncta and colocalization with autolysosomes, and upregulated the conversion of endogenous Lc3. PMC2754832
Mice DSS-induced colitis model intraperitoneal injection 5 mg/kg daily for 5 days To study the effect of Calpeptin on DSS-induced colitis in mice, results showed that Calpeptin treatment reduced weight loss and improved architectural distortion and epithelial cell death. PMC4362239
Mice SMA mouse models subcutaneous injection 6 μg/g once daily until postnatal day 8 To study the effect of Calpeptin on survival and motor function in SMA mice, results showed that Calpeptin treatment increased SMN protein levels and improved motor function PMC7316821
Mice C57BL/6J mice FemOral vein injection 20 mg/kg body weight Single injection, analyzed after 4 hours To study the effect of ApoA-I injection on ABCA1 protein levels in mouse liver and peritoneal macrophages, results showed that ApoA-I injection significantly increased ABCA1 protein levels. PMC151839

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.76mL

0.55mL

0.28mL

13.79mL

2.76mL

1.38mL

27.59mL

5.52mL

2.76mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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