2. Metabolic Enzyme/Protease
  3. Cathepsin
  4. CA-074 methyl ester

CA-074 methyl ester  (Synonyms: CA-074Me)

Cat. No.: HY-100350 Purity: 98.65%
COA Handling Instructions

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

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

CA-074 methyl ester Chemical Structure

CA-074 methyl ester Chemical Structure

CAS No. : 147859-80-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 126 In-stock
Solution
10 mM * 1 mL in DMSO USD 126 In-stock
Solid
1 mg USD 84 In-stock
5 mg USD 144 In-stock
10 mg USD 220 In-stock
25 mg USD 440 In-stock
50 mg   Get quote  
100 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 29 publication(s) in Google Scholar

CA-074 methyl ester Related Antibodies

Top Publications Citing Use of Products

    CA-074 methyl ester purchased from MedChemExpress. Usage Cited in: Sci Total Environ. 2023 Apr 13;163460.  [Abstract]

    CA-074 methyl ester (CA; 10 μM; 4 h) significantly reduces the benzo(a)pyrene (BaP) and dibutyl phthalate (DBP) co-exposure-induced expression of p62 and co-localization of p62 and LC3 in macrophages.

    CA-074 methyl ester purchased from MedChemExpress. Usage Cited in: Sci Total Environ. 2023 Apr 13;163460.  [Abstract]

    CA-074 methyl ester (CA; 10 μM; 4 h) remarkably mitigates the up-regulation of CTSB induced by benzo(a)pyrene (BaP) and dibutyl phthalate (DBP) co-exposure in macrophages.

    CA-074 methyl ester purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2020 Sep 15;201:110831.  [Abstract]

    Representative images of Western blotting in irradiated GC-1 cells pretreated with MG-132 (10 nM, 12 h) and CA-074me (10 μM, 12 h). The expression of Rpl27a is increased and p53 is decreased in the CA-074-me-treated CIR group.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    Cathepsin B

     

    In Vitro

    CA-074Me (5 μM and 50 μM) inhibits RANKL-induced osteoclastogenesis in BMM cells derived from C57BL/6J and NOD/ShiLtJ mice. CA-074Me exerts its anti-osteoclastogenic effect within 24 hours post-RANKL stimulation in vitro. CA-074Me does not exert its anti-osteoclastogenic effect via the MAPK-ERK signaling cascade. CA-074Me inhibits c-FOS upregulation and subsequent NFATc1 autoamplification following RANKL stimulation.[2].
    CA-074Me reduces apoptosis induced by CVB1[3].

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

    CA-074 methyl ester Related Antibodies
    In Vivo

    Hippocampal CA1 neuronal programmed necrosis induced by global cerebral I/R injury is prevented by CA074-me (1 μg, 10 μg) both pre-treatment and post-treatment. The rupture of lysosomal membrane and the leakage of cathepsin-B, and this is strongly inhibited by CA074-me pre-treatment. The overexpression and nuclear translocation of RIP3 and the reduction of NAD+ level after I/R injury are also inhibited, while the upregulation of Hsp70 is strengthened by CA074-me pre-treatment[1].
    CA-074Me (30 mg/kg) is capable of inhibiting osteoclastogenesis and bone degradation in vivo[2].
    In the CVB+CA-074Me (4 mg/kg/day i.m.) guinea pigs group, the scores of inflammation significantly decrease in comparison with the CVB+None group. In CVB+CA-074Me group, the number of CD8+T cells decrease in comparison with the sham group[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    397.47

    Formula

    C19H31N3O6
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C([C@@H]1[C@@H](C(NCCC)=O)O1)N[C@]([C@@H](C)CC)([H])C(N(CCC2)[C@@H]2C(OC)=O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (251.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5159 mL 12.5796 mL 25.1591 mL
    5 mM 0.5032 mL 2.5159 mL 5.0318 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.34%

    COA (246 KB) LCMS (88 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [2]

    After seven days of cell culture and osteoclast generation, the media is removed and washed three times with PBS. BMMs are fixed with a fixing solution supplied by the manufacturer. The cells are incubated at 37°C with a solution containing deionized water, Fast Garnet GBC, Napthol phosphate, Acetate, and Tartrate for 1 h. The staining solution is removed, washed with PBS (3×), and air-dried. TRAP positive cells with three or more nuclei across whole culture area are counted as multinucleated osteoclasts using light microscopy.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    RANKL (0.08 mg/kg) with and without CA-074Me (10 mg/kg or 30 mg/kg) are mixed in sterile, nonimmunogenic 1% Extracel-HP gel. The gel is composed of thiol-modified sodium hyaluronate, thiol-modified heparin, thiol-modified gelatin, and degassed deionized sterile water. The hydrogel mixture is prepared in an aseptic hood using a sterile syringe. The control sham hydrogel contained sterile Phosphate Buffered Saline (PBS) without any cytokines. The osteolysis group is given 0.08 mg/kg RANKL in a hydrogel to induce pathologic bone loss. The hydrogel-only, hydrogel-RANKL, and hydrogel-RANKL-CA-074Me mixture is injected into 8-week old male mice calvarium in an aseptic hood (n = 5) following general anesthesia (80 mg/kg of ketamine and 7 mg/kg of xylazine). After four days, the calvaria are excised, fixed in 4% formaldehyde for 24 h, decalcified in 20% EDTA for one week, and sectioned into slides from paraffin blocks. The slides undergo Tartrate-Resistant Acid Phosphatase (TRAP) staining to identify osteoclasts.

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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5159 mL 12.5796 mL 25.1591 mL 62.8978 mL
    5 mM 0.5032 mL 2.5159 mL 5.0318 mL 12.5796 mL
    10 mM 0.2516 mL 1.2580 mL 2.5159 mL 6.2898 mL
    15 mM 0.1677 mL 0.8386 mL 1.6773 mL 4.1932 mL
    20 mM 0.1258 mL 0.6290 mL 1.2580 mL 3.1449 mL
    25 mM 0.1006 mL 0.5032 mL 1.0064 mL 2.5159 mL
    30 mM 0.0839 mL 0.4193 mL 0.8386 mL 2.0966 mL
    40 mM 0.0629 mL 0.3145 mL 0.6290 mL 1.5724 mL
    50 mM 0.0503 mL 0.2516 mL 0.5032 mL 1.2580 mL
    60 mM 0.0419 mL 0.2097 mL 0.4193 mL 1.0483 mL
    80 mM 0.0314 mL 0.1572 mL 0.3145 mL 0.7862 mL
    100 mM 0.0252 mL 0.1258 mL 0.2516 mL 0.6290 mL
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    CA-074 methyl ester Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    CA-074 methyl ester147859-80-1CA-074MeCathepsinInhibitorinhibitorinhibit

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