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

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

Cat. No.: HY-100350 Purity: 99.15%
Handling Instructions

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

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10 mM * 1 mL in DMSO USD 126 In-stock
Estimated Time of Arrival: December 31
1 mg USD 84 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 252 In-stock
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25 mg USD 492 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

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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.

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].

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].

Molecular Weight

397.47

Formula

C₁₉H₃₁N₃O₆

CAS No.

147859-80-1

SMILES

O=C([[email protected]@H]1[[email protected]@H](C(NCCC)=O)O1)N[[email protected]]([[email protected]@H](C)CC)([H])C(N(CCC2)[[email protected]@H]2C(OC)=O)=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 : ≥ 215 mg/mL (540.92 mM)

H2O : 26.66 mg/mL (67.07 mM; Need warming)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.2516 mL 1.2580 mL 2.5159 mL
*Please refer to the solubility information to select the appropriate solvent.
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

Purity: 99.15%

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Keywords:

CA-074 methyl esterCA-074MeCathepsinInhibitorinhibitorinhibit

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CA-074 methyl ester
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HY-100350
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