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Chemical Structure| 147859-80-1 Chemical Structure| 147859-80-1
Chemical Structure| 147859-80-1

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CAS No.: 147859-80-1

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CA-074 methyl ester is a specific inhibitor of Cathepsin B, which possesses potent bioactivities such as neuroprotective, anti-cancer, and anti-inflammatory effects.

Synonyms: CA-074Me; Cathepsin B Inhibitor IV

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Product Details of CA-074 methyl ester

CAS No. :147859-80-1
Formula : C19H31N3O6
M.W : 397.47
SMILES Code : O=C(OC)[C@H]1N(C([C@H]([C@@H](C)CC)NC([C@H]2O[C@@H]2C(NCCC)=O)=O)=O)CCC1
Synonyms :
CA-074Me; Cathepsin B Inhibitor IV
MDL No. :MFCD03452890
InChI Key :XGWSRLSPWIEMLQ-YTFOTSKYSA-N
Pubchem ID :6610318

Safety of CA-074 methyl ester

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of CA-074 methyl ester

pyroptosis

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description Reference
ACE2-expressing iPS cells 10 μM 4 days CA-074 Me treatment reduced the viral RNA copy number to 0.62% ±0.25%, indicating its effective inhibition of SARS-CoV-2 infection PMC8527102
RAW 264.7 macrophages 20 μM 36 hours CA-074-me effectively reversed hemin-induced cell death at concentrations higher than 10 μM, with 20 μM showing the best therapeutic effect. PMC10796092
mouse peritoneal macrophages 25 μM 1-hour pretreatment followed by infection with V. alginolyticus for 12 hours Inhibited NLRP3 inflaμMasome activation and reduced IL-1β secretion PMC8634873
Kupffer cells (KCs) 75 μM 1 h To evaluate the effect of CTSB and CTSS inhibitors on IL-12 mRNA expression in KCs, results showed that CTSB and CTSS inhibitors significantly reduced LPS-induced IL-12 mRNA expression. PMC5836516
RAW264.7 cells 75 μM 1 h To evaluate the effect of CTSB and CTSS inhibitors on NF-κB nuclear translocation in RAW264.7 cells, results showed that CTSB and CTSS inhibitors significantly reduced LPS-induced NF-κB nuclear translocation. PMC5836516
C1R-CD1d cells 75 μM 1 h To evaluate the effect of CTSB and CTSS inhibitors on α-GalCer antigen loading in C1R-CD1d cells, results showed that CTSS inhibitor significantly reduced iNKT cell activation, while CTSB inhibitor had no significant effect. PMC5836516
LX2 cells 75 μM 1 h To evaluate the effect of CTSB and CTSS inhibitors on α-GalCer antigen loading in LX2 cells, results showed that CTSS inhibitor significantly reduced iNKT cell activation, while CTSB inhibitor had no significant effect. PMC5836516
HKC-8 cells 10μM 48 hours To evaluate the inhibitory effect of CA-074 methyl ester on CtsB activity in HKC-8 cells, results showed that CA-074 methyl ester inhibited CtsB activity but had no effect on CtsD activity. PMC4735715

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
C57BL/6 mice Spinal cord injury model Tail vein injection 600 mg twice daily Twice daily, until May 2021 CA-074-me reduced lipid peroxidation and mitochondrial degeneration after spinal cord injury, promoting neurological function recovery. PMC10796092
Mice BTBR autism model Intracerebroventricular injection 300 mg/kg Twice daily for 4 days Inhibition of cathepsin B activity, reducing leukocyte-endothelial cell adhesion PMC6488924
Female C57BL/6J mice Age-induced spontaneous osteoarthritis model (AOA) Intra-articular injection 10 mg/kg Once daily for 14 days To evaluate the therapeutic effect of CA074me in an age-induced osteoarthritis model, results showed that the combination treatment improved pain hypersensitivity but did not significantly improve joint structure. PMC10813022
Rat Traumatic Brain Injury (TBI) model Intracerebroventricular infusion 600 μM in 5μL Twice a week for 4 weeks To evaluate the effects of CA-074Me following traumatic brain injury and secondary intracranial pressure elevation, results showed that CA-074Me reduced Cath B activity and alleviated sensory hypersensitivity. PMC11274534
Mice C57BL/6 male mice Intraperitoneal injection 100 mg/kg every 2 days for 2 weeks To evaluate the effect of CTSB and CTSS inhibitors on LPS or α-GalCer-induced iNKT cell activation and liver injury, results showed that CTSB and CTSS inhibitors significantly reduced iNKT cell activation and liver injury. PMC5836516
Mice Unilateral ureter obstruction (UUO) model Intraperitoneal injection 10 μg/μL Continuous for 2 weeks To evaluate the effect of CA-074 methyl ester on renal fibrosis in the UUO model, results showed that CA-074 methyl ester inhibited CtsB activity but had no significant effect on renal fibrosis. PMC4735715

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.58mL

2.52mL

1.26mL

25.16mL

5.03mL

2.52mL
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

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