Balicatib
Based on 2 publication(s) in Google Scholar
Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC50 values of 22, 61, 48, 2900 nM for cathepsin K, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis.
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- Pureza: 98.25%
- No. CAS: 354813-19-7
- Fòrmula: C23H33N5O2
- Peso molecular:411.54
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Balicatib
MoreVer todos los productos específicos de isoformas Cathepsin
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Actividad biológica
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cathepsin K 22 nM (IC50) |
cathepsin L 48 nM (IC50) |
Cathepsin B 61 nM (IC50) |
cathepsin S 2900 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A20 | IC50 |
6180 nM
Compound: 10
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Effect of compound on antigen presentation in mouse A20 cells transfected with PC-specific mIgM by IL-2 secretion
Effect of compound on antigen presentation in mouse A20 cells transfected with PC-specific mIgM by IL-2 secretion
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[PMID: 16302795] |
| HepG2 | IC50 |
48 nM
Compound: 10
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Inhibitory activity against human cathepsin L expressed in HepG2 cells
Inhibitory activity against human cathepsin L expressed in HepG2 cells
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[PMID: 16302795] |
| HepG2 | IC50 |
48 nM
Compound: balicatib
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Inhibition of cathepsin L in human HepG2 cells
Inhibition of cathepsin L in human HepG2 cells
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[PMID: 18226527] |
| HepG2 | IC50 |
61 nM
Compound: 10
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Inhibitory activity against human cathepsin B expressed in HepG2 cells
Inhibitory activity against human cathepsin B expressed in HepG2 cells
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[PMID: 16302795] |
| HepG2 | IC50 |
61 nM
Compound: balicatib
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Inhibition of cathepsin B in human HepG2 cells
Inhibition of cathepsin B in human HepG2 cells
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[PMID: 18226527] |
| Osteoclast | IC50 |
97 nM
Compound: 10
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Effect of compound on degradation of collagen in osteoclast bone resorption assay
Effect of compound on degradation of collagen in osteoclast bone resorption assay
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[PMID: 16302795] |
| Osteoclast | IC50 |
97 nM
Compound: balicatib
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Inhibition of bone resorption in rabbit osteoclast
Inhibition of bone resorption in rabbit osteoclast
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[PMID: 18226527] |
| Ramos | IC50 |
2900 nM
Compound: 10
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Inhibitory activity against human cathepsin S expressed in ramos cells
Inhibitory activity against human cathepsin S expressed in ramos cells
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[PMID: 16302795] |
| Ramos | IC50 |
2900 nM
Compound: balicatib
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Inhibition of cathepsin S in human ramos cells
Inhibition of cathepsin S in human ramos cells
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[PMID: 18226527] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:11-13 years, female cynomolgus monkeys (Macaca fascicularis)[1]
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Dosage:0, 3, 10, 50 mg/kg
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Administration:Oral gavage; twice daily for 18 months
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Result:Completely prevented ovariectomy-induced increases in BFR/BS in cancellous bone of vertebra and femur and in osteonal and endocortical bone of vertebra, significantly decreased bone formation rates.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 354813-19-7
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Appearance Solid
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Peso molecular 411.54
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Fòrmula C23H33N5O2
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Color White to off-white
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SMILES
CCCN1CCN(C2=CC=C(C(NC3(C(NCC#N)=O)CCCCC3)=O)C=C2)CC1
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Synonyms
AAE581
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Sci Rep
Hepatitis C virus NS3/4A inhibitors and other drug-like compounds as covalent binders of SARS-CoV-2 main protease. [Abstract]2022 Jul 16;12(1):12197. PMID: 35842458 -
iScience
Cathepsin K promotes the proliferation of hepatocellular carcinoma cells through induction of SIAH1 ubiquitination and degradation. [Abstract]2023 May 9;26(6):106852. PMID: 37250786
Solvente y solubilidad
DMSO : 75 mg/mL (182.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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: ≥ 3.75 mg/mL (9.11 mM); Clear solution
This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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: ≥ 3.75 mg/mL (9.11 mM); Clear solution
This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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.
Pureza y Documentación
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Ficha de datos (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Jerome C, et al. Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys. Osteoporos Int. 2012 Jan;23(1):339-49. [Content Brief]
[2]. Gauthier JY, et al. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. [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 | 2.4299 mL | 12.1495 mL | 24.2990 mL | 60.7474 mL |
| 5 mM | 0.4860 mL | 2.4299 mL | 4.8598 mL | 12.1495 mL | |
| 10 mM | 0.2430 mL | 1.2149 mL | 2.4299 mL | 6.0747 mL | |
| 15 mM | 0.1620 mL | 0.8100 mL | 1.6199 mL | 4.0498 mL | |
| 20 mM | 0.1215 mL | 0.6075 mL | 1.2149 mL | 3.0374 mL | |
| 25 mM | 0.0972 mL | 0.4860 mL | 0.9720 mL | 2.4299 mL | |
| 30 mM | 0.0810 mL | 0.4050 mL | 0.8100 mL | 2.0249 mL | |
| 40 mM | 0.0607 mL | 0.3037 mL | 0.6075 mL | 1.5187 mL | |
| 50 mM | 0.0486 mL | 0.2430 mL | 0.4860 mL | 1.2149 mL | |
| 60 mM | 0.0405 mL | 0.2025 mL | 0.4050 mL | 1.0125 mL | |
| 80 mM | 0.0304 mL | 0.1519 mL | 0.3037 mL | 0.7593 mL | |
| 100 mM | 0.0243 mL | 0.1215 mL | 0.2430 mL | 0.6075 mL |
Balicatib Related Classifications
HY-15100 Related Classifications
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