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CA-074

Cat. No. M6237
CA-074 Structure
Size Price Availability Quantity
5mg USD 260 In stock
10mg USD 380 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: CA-074 is a synthetic analogue of E-64, a natural peptidyl epoxide that irreversibly inhibits most known lysosomal cysteine proteinases, and is developed by means of rational drug design, exploiting the dipeptidylcarboxypeptidase activity of cathepsin B. CA-074 can be used to selectively inhibit cathepsin B within living cells, as long as the experimental conditions permit significant fluid-phase endocytosis of the drug. CA-074 inhibits cathepsin B with a Ki of 2 to 5 nM, whereas the initial Kis for cathepsin H and L are about 40-200 μM. CA-074 exhibits 10000-30000 times greater inhibitory effects on purified rat cathepsin B than on cathepsin H and L.

In vivo: Intraperitoneally injection of compound CA-074 into rats potently and selectively inhibits cathepsin B activity. Intravenously administration of CA-074 immediately after the ischaemic insult saves 67% of CA1 neurons from delayed neuronal death on day 5 in eight monkeys undergoing 20 min brain ischaemia: the extent of inhibition is excellent in three of eight and good in five of eight monkeys.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Rats
Formulation saline containing DMSO
Dosages 8 mg/100 g body weight
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 383.44
Formula C18H29N3O6
CAS Number 134448-10-5
Purity >98%
Solubility 150 mg/mL in DMSO
Storage at -20°C
References

Distinct cathepsins control necrotic cell death mediated by pyroptosis inducers and lysosome-destabilizing agents.
Brojatsch J, et al. Cell Cycle. 2015;14(7):964-72. PMID: 25830414.

A proteolytic cascade controls lysosome rupture and necrotic cell death mediated by lysosome-destabilizing adjuvants.
Brojatsch J, et al. PLoS One. 2014 Jun 3;9(6):e95032. PMID: 24893007.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CA-074 supplier, Caspase, inhibitors

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