L-873724
Based on 1 Customer Validation
L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also exhibits an IC50 of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.93%
- No. CAS: 603139-12-4
- Fòrmula: C23H26F3N3O3S
- Peso molecular:481.53
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
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Cathepsin B |
cathepsin K |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
1221 nM
Compound: 22
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Potency against Cathepsin L in HepG2 cells by whole cell enzyme occupancy assay
Potency against Cathepsin L in HepG2 cells by whole cell enzyme occupancy assay
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[PMID: 16413777] |
| HepG2 | IC50 |
1221 nM
Compound: L-873724
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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 |
4807 nM
Compound: 22
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Potency against Cathepsin B in HepG2 cells by whole cell enzyme occupancy assay
Potency against Cathepsin B in HepG2 cells by whole cell enzyme occupancy assay
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[PMID: 16413777] |
| HepG2 | IC50 |
4807 nM
Compound: L-873724
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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 |
13 nM
Compound: 22
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Activity in rabbit osteoclasts by bone resorption assay
Activity in rabbit osteoclasts by bone resorption assay
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[PMID: 16413777] |
| Osteoclast | IC50 |
13 nM
Compound: L-873724
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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 |
95 nM
Compound: 22
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Potency against Cathepsin S in Ramos cells by whole cell enzyme occupancy assay
Potency against Cathepsin S in Ramos cells by whole cell enzyme occupancy assay
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[PMID: 16413777] |
| Ramos | IC50 |
95 nM
Compound: L-873724
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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] |
In Vitro
L-873724 (Compound 22) is a potent and selective non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also shows IC50s of 95, 1221 and 4807 nM for Ramos cathepsin S, Hep G2 cathepsin L, Hep G2 cathepsin B[1]. L-873724 exhibits an IC50 of 0.5 nM for rabbit cathepsin K[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 603139-12-4
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Appearance Solid
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Peso molecular 481.53
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Fòrmula C23H26F3N3O3S
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Color White to off-white
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SMILES
O=S(C1=CC=C(C2=CC=C([C@@H](C(F)(F)F)N[C@@H](CC(C)C)C(NCC#N)=O)C=C2)C=C1)(C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (207.67 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.19 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 (5.19 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:
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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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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
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Osteoclast differentiation from monocyte/macrophage precursors
Osteoclast differentiation is an in vitro induction assay in which monocyte/macrophage-lineage precursors are exposed to macrophage colony-stimulating factor (M-CSF) and receptor activator of NF-κB ligand (RANKL), generating multinucleated osteoclasts that are commonly identified by tartrate-resistant acid phosphatase (TRAP) staining and functionally confirmed by resorption pits on dentin, bone, or mineralized substrates. M-CSF supports survival and expansion of osteoclast precursors, while RANKL binding to RANK drives osteoclast commitment, fusion, maturation, and resorptive function; osteoprotegerin inhibits this pathway by binding RANKL and preventing RANK activation. The main readouts are the number of TRAP-positive multinucleated cells, formation of F-actin rings, and resorbed surface area; TRAP-positive multinucleated cells indicate osteoclast differentiation, whereas pit formation on dentin, bone, or mineralized coating indicates functional bone-resorbing activity.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Li CS, et al. Identification of a potent and selective non-basic cathepsin K inhibitor. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1985-9. [Content Brief]
[2]. Zhuo Y, et al. Inhibition of bone resorption by the cathepsin K inhibitor odanacatib is fully reversible. Bone. 2014 Oct;67:269-80. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0767 mL | 10.3836 mL | 20.7671 mL | 51.9178 mL |
| 5 mM | 0.4153 mL | 2.0767 mL | 4.1534 mL | 10.3836 mL | |
| 10 mM | 0.2077 mL | 1.0384 mL | 2.0767 mL | 5.1918 mL | |
| 15 mM | 0.1384 mL | 0.6922 mL | 1.3845 mL | 3.4612 mL | |
| 20 mM | 0.1038 mL | 0.5192 mL | 1.0384 mL | 2.5959 mL | |
| 25 mM | 0.0831 mL | 0.4153 mL | 0.8307 mL | 2.0767 mL | |
| 30 mM | 0.0692 mL | 0.3461 mL | 0.6922 mL | 1.7306 mL | |
| 40 mM | 0.0519 mL | 0.2596 mL | 0.5192 mL | 1.2979 mL | |
| 50 mM | 0.0415 mL | 0.2077 mL | 0.4153 mL | 1.0384 mL | |
| 60 mM | 0.0346 mL | 0.1731 mL | 0.3461 mL | 0.8653 mL | |
| 80 mM | 0.0260 mL | 0.1298 mL | 0.2596 mL | 0.6490 mL | |
| 100 mM | 0.0208 mL | 0.1038 mL | 0.2077 mL | 0.5192 mL |
L-873724 Related Classifications
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