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> CA-074 methyl ester [147859-80-1]

CA-074 methyl ester [147859-80-1]

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Cat# HY-100350-1ml

Size : 10mM/1mL

Brand : MedChemExpress

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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)(11)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.

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.
Purity & Documentation
References

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