CA-074 methyl ester
Based on 46 publication(s) in Google Scholar
CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.81%
- No. CAS: 147859-80-1
- Fòrmula: C19H31N3O6
- Peso molecular:397.47
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) CA-074 methyl ester
More- Signal Transduct Target Ther. 2025 Sep 26;10(1):310. [Abstract]
- Cell Mol Immunol. 2020 Mar;17(3):283-299. [Abstract]
- Adv Funct Mater. 2023 Apr 28.
- Transl Neurodegener. 2026 Jun 28;15(1):29. [Abstract]
- ACS Nano. 2026 May 5;20(17):13196-13212. [Abstract]
- Redox Biol. 2026 Mar:90:104059. [Abstract]
- Theranostics. 2021 Oct 11;11(20):9821-9832. [Abstract]
- J Clin Invest. 2026 Feb 17:e194139. [Abstract]
- Sci Adv. 2022 Nov 11;8(45):eabn9912. [Abstract]
- Cell Death Dis. 2026 May 30. [Abstract]
- Environ Sci Technol. 2017 Dec 5;51(23):13938-13948. [Abstract]
- Biosens Bioelectron. 2025 Jan 25:274:117184. [Abstract]
- J Hazard Mater. 2024 Apr 5:467:133719. [Abstract]
- Int J Biol Macromol. 2024 Sep 23:135876. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2026 May 12:101810. [Abstract]
- Cell Rep. 2025 Aug 21;44(9):116186. [Abstract]
- Emerg Microbes Infect. 2022 Dec;11(1):483-497. [Abstract]
- J Agric Food Chem. 2023 May 10;71(18):7032-7045. [Abstract]
- Ecotoxicol Environ Saf. 2020 Sep 15;201:110831. [Abstract]
- Mol Ther Nucleic Acids. 2025 Sep 30;36(4):102726. [Abstract]
- Cell Mol Life Sci. 2022 Jun 11;79(7):360. [Abstract]
- RSC Adv. 2021 May 6;11(27):16522-16529. [Abstract]
- Commun Biol. 2025 Jul 23;8(1):1097. [Abstract]
- Commun Biol. 2025 Jun 2;8(1):845. [Abstract]
- Int Immunopharmacol. 2026 Jul 1:180:116695. [Abstract]
- Int Immunopharmacol. 2020 Nov;88:106985. [Abstract]
- Mol Neurobiol. 2025 May 30. [Abstract]
- Mol Pharm. 2024 May 9. [Abstract]
- Mol Cell Biochem. 2025 Jun;480(6):3889-3906. [Abstract]
- iScience. 2024 Oct 4;27(11):111024. [Abstract]
- Biosci Rep. 2019 Jul 2;39(7):BSR20190516. [Abstract]
- J Virol. 2025 Aug 11:e0105525. [Abstract]
- J Immunol. 2026 Mar 17;215(3):vkag020. [Abstract]
- Neurotoxicology. 2026 Apr 28:103462. [Abstract]
- Viruses. 2021 May 31;13(6):1035. [Abstract]
- Toxicol Appl Pharmacol. 2026 Jan:506:117632. [Abstract]
- PLoS Negl Trop Dis. 2021 Apr 2;15(4):e0009304. [Abstract]
- Toxicol Appl Pharmacol. 2018 Oct 1;356:159-171. [Abstract]
- Bioorg Med Chem. 2020 Jul 1;28(13):115547 [Abstract]
- Food Chem Toxicol. 2024 Mar:185:114431. [Abstract]
- bioRxiv. 2024 November 23.
- bioRxiv. 2024 July 03.
- Preprints. 2024 May 27.
- Virginia Commonwealth University. 2023 Aug.
- Sci Total Environ. 2023 Jul 10:881:163460. [Abstract]
- Research Square Preprint. 2021 Mar.
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Ver todos los productos específicos de isoformas Cathepsin
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Actividad biológica
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Cathepsin B |
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-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.
Chemical Information
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No. CAS 147859-80-1
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Appearance Solid
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Peso molecular 397.47
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Fòrmula C19H31N3O6
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Color White to off-white
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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
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Synonyms
CA-074Me
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 2 years -20°C 1 year
Publications (46)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Reprogramming of cancer metabolism via photoresponsive nano-PROTAC enhances pyroptosis-mediated immunotherapy. [Abstract]2025 Sep 26;10(1):310. PMID: 40998785 -
Cell Mol Immunol
2020 Mar;17(3):283-299. PMID: 31320730 -
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Transl Neurodegener
2026 Jun 28;15(1):29. PMID: 42365390 -
ACS Nano
Combinatorial Design of Fatty Acid-Incorporated Plasmid Lipid Nanoparticles Drives Dendritic Cell Hyperactivation for Enhanced Cancer Immunotherapy. [Abstract]2026 May 5;20(17):13196-13212. PMID: 42003370 -
Redox Biol
Lactate-driven ATP6V1B2 lactylation triggers asthmatic inflammation by linking lysosomal dysfunction to mitochondrial ROS-dependent pyroptosis. [Abstract]2026 Mar:90:104059. PMID: 41637881 -
Theranostics
CST6 protein and peptides inhibit breast cancer bone metastasis by suppressing CTSB activity and osteoclastogenesis. [Abstract]2021 Oct 11;11(20):9821-9832. PMID: 34815788 -
J Clin Invest
Galectin-3 mediates lysosome-related inflammation within monocyte-derived macrophages in a mouse model of ischemic brain injury. [Abstract]2026 Feb 17:e194139. PMID: 41701549 -
Sci Adv
Caspase-8 inactivation drives autophagy-dependent inflammasome activation in myeloid cells. [Abstract]2022 Nov 11;8(45):eabn9912. PMID: 36367942 -
Cell Death Dis
CLN7 suppression induces apoptosis via mTOR-regulated and chaperone-mediated autophagy in myeloid leukemia cells. [Abstract]2026 May 30. PMID: 42218124 -
Environ Sci Technol
Determining the Cytotoxicity of Rare Earth Element Nanoparticles in Macrophages and the Involvement of Membrane Damage. [Abstract]2017 Dec 5;51(23):13938-13948. PMID: 29121463 -
Biosens Bioelectron
Cathepsin B dependent activatable trigger fluorophore (CAT-Fluor) for in situ functional imaging of antibody-drug conjugates. [Abstract]2025 Jan 25:274:117184. PMID: 39879789 -
J Hazard Mater
Sodium sulfite triggered hepatic apoptosis, necroptosis, and pyroptosis by inducing mitochondrial damage in mice and AML-12 cells. [Abstract]2024 Apr 5:467:133719. PMID: 38335615 -
Int J Biol Macromol
Duck hepatitis A virus 1-encoded 2B protein disturbs ion and organelle homeostasis to promote NF-κB/NLRP3-mediated inflammatory response. [Abstract]2024 Sep 23:135876. PMID: 39322136 -
Cell Mol Gastroenterol Hepatol
Kupffer Cell-Derived Exosomal S100A8/A9 Promotes Inflammasome-Dependent Pyroptotic Lung Injury in Acute Pancreatitis. [Abstract]2026 May 12:101810. PMID: 42128052 -
Cell Rep
TCF25 serves as a nutrient sensor to orchestrate metabolic adaptation and cell death by enhancing lysosomal acidification under glucose starvation. [Abstract]2025 Aug 21;44(9):116186. PMID: 40844875 -
Emerg Microbes Infect
Obatoclax inhibits SARS-CoV-2 entry by altered endosomal acidification and impaired cathepsin and furin activity in vitro. [Abstract]2022 Dec;11(1):483-497. PMID: 34989664 -
J Agric Food Chem
Apigenin Alleviated High-Fat-Diet-Induced Hepatic Pyroptosis by Mitophagy-ROS-CTSB-NLRP3 Pathway in Mice and AML12 Cells. [Abstract]2023 May 10;71(18):7032-7045. PMID: 37141464 -
Ecotoxicol Environ Saf
Heavy ion radiation-induced DNA damage mediates apoptosis via the Rpl27a-Rpl5-MDM2-p53/E2F1 signaling pathway in mouse spermatogonia. [Abstract]2020 Sep 15;201:110831. PMID: 32535367
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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Mol Ther Nucleic Acids
SARS-CoV-2 infection in hiPSC-derived neurons is cathepsin-dependent and causes differential accumulation of HIF1ɑ and phosphorylated tau. [Abstract]2025 Sep 30;36(4):102726. PMID: 41216428 -
Cell Mol Life Sci
Phenazine derivatives attenuate the stemness of breast cancer cells through triggering ferroptosis. [Abstract]2022 Jun 11;79(7):360. PMID: 35690642 -
RSC Adv
IQF characterization of a cathepsin B-responsive nanoprobe for report of differentiation of HL60 cells into macrophages. [Abstract]2021 May 6;11(27):16522-16529. PMID: 35479137 -
Commun Biol
Cathepsin B deficiency disrupts cortical development via PEG3, leading to depression-like behavior. [Abstract]2025 Jul 23;8(1):1097. PMID: 40702210 -
Commun Biol
Cathepsin B-dependent glycolysis contributes to reduced renal uric acid excretion in hyperuricemia. [Abstract]2025 Jun 2;8(1):845. PMID: 40457023 -
Int Immunopharmacol
Cathepsin B regulated via TFEB and lysosomal membrane permeabilization in adipose tissue macrophages aggravates obesity-related severe acute pancreatitis. [Abstract]2026 Jul 1:180:116695. PMID: 42019387 -
Int Immunopharmacol
IL-6 promotes collagen-induced arthritis by activating the NLRP3 inflammasome through the cathepsin B/S100A9-mediated pathway. [Abstract]2020 Nov;88:106985. PMID: 33182050 -
Mol Neurobiol
Inhibition of Cathepsin B Ameliorates Murine Cognitive Dysfunction and Neuronal Damage in Ischemic Stroke by Inhibiting Mitochondrial Apoptosis and Drp1-Mediated Mitochondrial Fission. [Abstract]2025 May 30. PMID: 40447852 -
Mol Pharm
Saponin and Ribosome-Inactivating Protein Synergistically Trigger Lysosome-Dependent Apoptosis by Inhibiting Lysophagy: Potential to Become a New Antitumor Strategy. [Abstract]2024 May 9. PMID: 38722865 -
Mol Cell Biochem
The molecular mechanism by which CTSB degrades FPN to disrupt macrophage iron homeostasis and promote the progression of atherosclerosis. [Abstract]2025 Jun;480(6):3889-3906. PMID: 39960586 -
iScience
Inhibition of cathepsin L ameliorates inflammation through the A20/NF-κB pathway in endotoxin-induced acute lung injury. [Abstract]2024 Oct 4;27(11):111024. PMID: 39559762 -
Biosci Rep
CaMKII/proteasome/cytosolic calcium/cathepsin B axis was present in tryspin activation induced by nicardipine. [Abstract]2019 Jul 2;39(7):BSR20190516. PMID: 31221819 -
J Virol
Cathepsin L and transmembrane serine protease 11E mediate trypsin-independent entry of porcine deltacoronavirus into Huh7 cells. [Abstract]2025 Aug 11:e0105525. PMID: 40787987 -
J Immunol
Cathepsin B promotes asthma potentially via macrophage-associated autophagy and apoptosis. [Abstract]2026 Mar 17;215(3):vkag020. PMID: 41847863 -
Neurotoxicology
Lysosomal dysfunction contributes to lead (Pb) and high-fat diet (HFD)-induced neuronal apoptosis: A link with cathepsin B. [Abstract]2026 Apr 28:103462. PMID: 42061594 -
Viruses
Bovine Parainfluenza Virus Type 3 (BPIV3) Enters HeLa Cells via Clathrin-Mediated Endocytosis in a Cholesterol- and Dynamin-Dependent Manner. [Abstract]2021 May 31;13(6):1035. PMID: 34072688 -
Toxicol Appl Pharmacol
Honokiol ameliorates hepatic fibrosis by inducing lysosomal membrane permeabilization and impairing lipophagy in hepatic stellate cells. [Abstract]2026 Jan:506:117632. PMID: 41207513 -
PLoS Negl Trop Dis
Extracellular vesicles secreted by Giardia duodenalis regulate host cell innate immunity via TLR2 and NLRP3 inflammasome signaling pathways. [Abstract]2021 Apr 2;15(4):e0009304. PMID: 33798196 -
Toxicol Appl Pharmacol
Alantolactone induces apoptosis and improves chemosensitivity of pancreatic cancer cells by impairment of autophagy-lysosome pathway via targeting TFEB. [Abstract]2018 Oct 1;356:159-171. PMID: 30086361 -
Bioorg Med Chem
Broad assessment of bioactivity of a collection of spiroindane pyrrolidines through "cell painting". [Abstract]2020 Jul 1;28(13):115547 PMID: 32546297 -
Food Chem Toxicol
Cell death induced by nicotine in human neuroblastoma SH-SY5Y cells is mainly attributed to cytoplasmic vacuolation originating from the trans-Golgi network. [Abstract]2024 Mar:185:114431. PMID: 38176581 -
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Sci Total Environ
Combined exposure to benzo(a)pyrene and dibutyl phthalate aggravates pro-inflammatory macrophage polarization in spleen via pyroptosis involving cathepsin B. [Abstract]2023 Jul 10:881:163460. PMID: 37061049
CA-074 methyl ester purchased from MedChemExpress. Usage Cited in: Sci Total Environ. 2023 Jul 10:881:163460. [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: Sci Total Environ. 2023 Jul 10:881:163460. [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.
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Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Xu Y, et al. Protective mechanisms of CA074-me (other than cathepsin-B inhibition) against programmed necrosis induced by global cerebral ischemia/reperfusion injury in rats. Brain Res Bull. 2016 Jan;120:97-105 [Content Brief]
[2]. Patel N, et al. CA-074Me compound inhibits osteoclastogenesis via suppression of the NFATc1 and c-FOS signaling pathways. J Orthop Res. 2015 Oct;33(10):1474-86 [Content Brief]
[3]. Zhang L, et al. Treatment with CA-074Me, a Cathepsin B inhibitor, reduces lung interstitial inflammation and fibrosis in a rat model of polymyositis. Lab Invest. 2015 Jan;95(1):65-77 [Content Brief]
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 |
CA-074 methyl ester Related Classifications
HY-100350 Related Classifications
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