| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
L006235 targets cathepsin K, a lysosomal cysteine protease that is predominantly expressed in osteoclasts and plays a critical role in bone resorption. Cathepsin K degrades the organic matrix of bone, primarily collagen type I. By inhibiting cathepsin K with high potency (IC₅₀ = 0.25 nM) and selectivity, L006235 prevents the degradation of bone matrix, thereby reducing bone resorption and preventing bone loss.
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| ln Vitro |
In the rabbit bone resorption experiment, L-006235 inhibits bone resorption with an IC50 of 5 nM[1]. In HepG2 cells, L-006235 (10 μM; 1 h) exhibits punctate fluorescence throughout the cytoplasm [2].
In vitro, L006235 is a potent inhibitor of cathepsin K with an IC₅₀ of 0.25 nM. In bone resorption assays, it has an IC₅₀ of 5 nM. It displays >4000-fold selectivity over cathepsins B, L, and S. These in vitro activities confirm its high potency and selectivity for cathepsin K, making it an excellent tool for studying the enzyme's function. |
| ln Vivo |
L-006235, a suggested share nutrient, decreases N-telopeptide (NTx) and creatine nutrient (Cre) in rhesus monkeys by up to 76% when administered poqd for 8-11 days [1]. L-006235 (20 mg/kg; po; deposition) has a lengthy terminal half-life (204 minutes), a high bioavailability (68%), and a Cmax (1.4 μM) [1].
In vivo, L006235 is an orally active cathepsin K inhibitor that can reduce collagen degradation and prevent bone loss. Its oral bioavailability and potent activity make it a promising candidate for the treatment of osteoporosis and other bone resorption diseases. Detailed in vivo efficacy data from specific animal models are not extensively reported in the available literature. |
| Enzyme Assay |
Non-cell-based enzyme assays for L006235 typically involve in vitro cathepsin K activity assays using purified recombinant cathepsin K enzyme. The compound is incubated with the enzyme and a fluorogenic substrate at varying concentrations. Cathepsin K activity is measured by monitoring the release of a fluorescent signal. IC₅₀ values, such as the 0.25 nM for cathepsin K inhibition, are determined from dose-response curves. Selectivity profiling against cathepsins B, L, and S is performed to confirm specificity.
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| Cell Assay |
Cellular assays for L006235 are performed using osteoclast cultures to assess its effects on bone resorption. Osteoclasts are cultured on bone slices or synthetic substrates and treated with the compound at various concentrations. Bone resorption is measured by quantifying the release of calcium or the formation of resorption pits. IC₅₀ values, such as the 5 nM in bone resorption assays, are determined.
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| Animal Protocol |
Animal/Disease Models: Rhesus monkey (15 years old) underwent ovariectomy (OVX) [1]
Doses: 0.6, 3, 15 mg/kg Route of Administration: Orally one time/day for 8-11 days Experimental Results: Average reduction in uNTx/Cre The 76%, 68% and 31% doses were 15, 3 and 0.6mg/kg respectively. In vivo animal models for L006235 include ovariectomized (OVX) rat models of osteoporosis, where the compound is administered orally at various doses. Efficacy is assessed by measuring bone mineral density, bone turnover markers, and bone histomorphometry. These studies confirm the compound's ability to reduce bone resorption and prevent bone loss. |
| ADME/Pharmacokinetics |
L006235 has a molecular weight of 466.60 g/mol and a molecular formula of C₂₄H₃₀N₆O₂S. Its CAS number is 294623-49-7. The compound is supplied as a solid with a purity of ≥99.74%. It is soluble in DMSO, but not in water. Storage conditions: -20°C. The compound is an orally active cathepsin K inhibitor. Detailed pharmacokinetic parameters such as half-life and bioavailability are not extensively reported.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for L006235 are not extensively reported in the available literature. As a research compound, its safety profile would need to be established through standard preclinical toxicity assessments. The compound is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
L006235 is also known as L-235. It is a potent, selective, reversible, and orally active inhibitor of cathepsin K with an IC₅₀ of 0.25 nM. In bone resorption assays, it has an IC₅₀ of 5 nM. It displays >4000-fold selectivity over cathepsins B, L, and S. L006235 can reduce collagen degradation and prevent bone loss. Its CAS number is 294623-49-7.
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| Molecular Formula |
C24H30N6O2S
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|---|---|
| Molecular Weight |
466.6
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| Exact Mass |
466.215
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| CAS # |
294623-49-7
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| PubChem CID |
9912381
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| Appearance |
White to off-white solid powder
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| LogP |
3.868
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
33
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| Complexity |
733
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FIVYCSWOCXEWSE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H30N6O2S/c1-29-13-15-30(16-14-29)23-27-20(17-33-23)18-5-7-19(8-6-18)21(31)28-24(9-3-2-4-10-24)22(32)26-12-11-25/h5-8,17H,2-4,9-10,12-16H2,1H3,(H,26,32)(H,28,31)
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| Chemical Name |
N-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
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| Synonyms |
L-006235; L 006235; L006235
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~31.25 mg/mL (~66.97 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.46 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.46 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1432 mL | 10.7158 mL | 21.4316 mL | |
| 5 mM | 0.4286 mL | 2.1432 mL | 4.2863 mL | |
| 10 mM | 0.2143 mL | 1.0716 mL | 2.1432 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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