1. Metabolic Enzyme/Protease
  2. Cathepsin
  3. CA-074

CA-074 

Cat. No.: HY-103350 Purity: 99.85%
Handling Instructions

CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.

For research use only. We do not sell to patients.

CA-074 Chemical Structure

CA-074 Chemical Structure

CAS No. : 134448-10-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 273 In-stock
Estimated Time of Arrival: December 31
1 mg USD 108 In-stock
Estimated Time of Arrival: December 31
5 mg USD 324 In-stock
Estimated Time of Arrival: December 31
10 mg USD 468 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.

IC50 & Target

Ki: 2 to 5 nM (Cathepsin B)[1]

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[2]. 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[1].

In Vivo

Intraperitoneally injection of compound CA-074 into rats potently and selectively inhibits cathepsin B activity[1]. 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[3].

Molecular Weight

383.44

Formula

C₁₈H₂₉N₃O₆

CAS No.

134448-10-5

SMILES

O=C(N1[[email protected]@H](CCC1)C(O)=O)[[email protected]@]([[email protected]@H](C)CC)([H])NC([[email protected]@H]2[[email protected]@H](C(NCCC)=O)O2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (326.00 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6080 mL 13.0399 mL 26.0797 mL
5 mM 0.5216 mL 2.6080 mL 5.2159 mL
10 mM 0.2608 mL 1.3040 mL 2.6080 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.42 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.42 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.42 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Rats: Compound CA-074 or CA-030 or E-64 is injected intraperitoneally as a solution in saline containing DMSO. A dose of 8 mg/100 g body weight is injected. The rats are killed by a blow to the head 6 h after the injection, and their liver is perfused with saline, removed, weighed and chilled on ice. Samples of 4 g of liver are minced and homogenized. The homogenate is centrifuged at 800 xg for 15 min and the supernatant is centrifuged at 12000 xg for 30 min. The precipitate is suspended in 2 mL of 0.05 M acetate buffer, pH 5,0, and freeze-thawed for measurements of cathepsin B, H and L activities[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.85%

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Keywords:

CA-074CA074CA 074CathepsinInhibitorinhibitorinhibit

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CA-074
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HY-103350
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