L-006235
Based on 1 Customer Validation
L-006235 (L-235) is a potent, selective, reversible and orally active inhibitor of cathepsin K, with an IC50 of 5 nM in bone resorption assay. L-006235 shows selectivity for cathepsin K (Ki=0.2 nM) over cathepsin B, cathepsin L, and cathepsin S (Ki=1, 6, and 47 μM, respectively). L-006235 can reduce collagen degradation and prevent bone loss.
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- Purity: 99.74%
- CAS No.: 294623-49-7
- 화학식: C24H30N6O2S
- 분자량:466.60
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Metabolism/Protease Compound Library
HY-L012
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Covalent Screening Library
HY-L036
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Orally Active Compound Library
HY-L061
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Angiogenesis-Related Compound Library
HY-L088
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Targeted Diversity Library
HY-L099
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Human Metabolite Library
HY-L123
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Coagulation and Anti-coagulation Compound Library
HY-L136
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Heterocyclic Compound Library
HY-L138
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Protease Inhibitor Library
HY-L147
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Highly Selective Inhibitors Library
HY-L158
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Multi-Target Compound Library
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Bioactive Compound Library Max
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MCE Bioactive Compound Library
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Covalent Screening Library Plus
HY-L036P
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Mass Spectrometry Human Metabolite Library
HY-L215
All Cathepsin Isoforms
More
Biological Activity
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Cathepsin B |
cathepsin K |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A20 | IC50 |
6200 nM
Compound: L-006235 1
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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 |
17 nM
Compound: L-006235 1
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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 |
340 nM
Compound: L-006235 1
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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] |
| Osteoclast | IC50 |
0.005 μM
Compound: 39n
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In vitro bone resorption in isolated rabbit osteoclasts
In vitro bone resorption in isolated rabbit osteoclasts
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[PMID: 16302794] |
| Osteoclast | IC50 |
5 nM
Compound: L-006235 1
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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] |
| Ramos | IC50 |
790 nM
Compound: L-006235 1
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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] |
L-006235 inhibits bone resorption in the rabbit bone resorption assay, with an IC50 of 5 nM[1].
L-006235 (10 μM; 1 h) show a punctate fluorescence throughout the cytoplasm in HepG2 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
L-006235 (20 mg/kg; p.o.) exhibits high oral bioavailability (68%), long terminal half-life (204 min) and Cmax (1.4 μM) in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rhesus monkey (15 years) receiving oophorectomy (OVX)[1]
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Dosage:0.6, 3, 15 mg/kg
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Administration:P.o once daily for 8-11 days
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Result:Decreased uNTx/Cre by an average of 76%, 68%, and 31% at the dose of 15, 3, and 0.6 mg/kg, respectively.
Chemical Information
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CAS No. 294623-49-7
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Appearance Solid
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분자량 466.60
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화학식 C24H30N6O2S
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Color White to off-white
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SMILES
O=C(NC1(C(NCC#N)=O)CCCCC1)C2=CC=C(C3=CSC(N4CCN(C)CC4)=N3)C=C2
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Synonyms
L-235
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 31.25 mg/mL (66.97 mM; ultrasonic and warming and heat to 60°C; 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. 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. 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)
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: ≥ 2.08 mg/mL (4.46 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.46 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
순도&문서
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Data Sheet (274 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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Handling Instructions (2659 KB)
References
[1]. Palmer JT, et, al. Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K. J Med Chem. 2005 Dec 1;48(24):7520-34. [Content Brief]
[2]. Falgueyret JP, et, al. Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J Med Chem. 2005 Dec 1;48(24):7535-43. [Content Brief]
[3]. Pennypacker BL, et, al. Cathepsin K inhibitors prevent bone loss in estrogen-deficient rabbits. J Bone Miner Res. 2011 Feb;26(2):252-62. [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. 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 | 2.1432 mL | 10.7158 mL | 21.4316 mL | 53.5791 mL |
| 5 mM | 0.4286 mL | 2.1432 mL | 4.2863 mL | 10.7158 mL | |
| 10 mM | 0.2143 mL | 1.0716 mL | 2.1432 mL | 5.3579 mL | |
| 15 mM | 0.1429 mL | 0.7144 mL | 1.4288 mL | 3.5719 mL | |
| 20 mM | 0.1072 mL | 0.5358 mL | 1.0716 mL | 2.6790 mL | |
| 25 mM | 0.0857 mL | 0.4286 mL | 0.8573 mL | 2.1432 mL | |
| 30 mM | 0.0714 mL | 0.3572 mL | 0.7144 mL | 1.7860 mL | |
| 40 mM | 0.0536 mL | 0.2679 mL | 0.5358 mL | 1.3395 mL | |
| 50 mM | 0.0429 mL | 0.2143 mL | 0.4286 mL | 1.0716 mL | |
| 60 mM | 0.0357 mL | 0.1786 mL | 0.3572 mL | 0.8930 mL |
L-006235 Related Classifications
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