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CathepsinK-IN-9 is a selective, potent, and orally active Cathepsin K inhibitor with an IC50 of 6.2 nM. It exhibits an IC50 greater than 10000 nM against cathepsins B, L, and S, demonstrating over 1600-fold selectivity. CathepsinK-IN-9 also displays excellent safety and metabolic stability, making it suitable for osteoporosis research.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | CathepsinK-IN-9 is a selective, potent, and orally active Cathepsin K inhibitor with an IC50 of 6.2 nM. It exhibits an IC50 greater than 10000 nM against cathepsins B, L, and S, demonstrating over 1600-fold selectivity. CathepsinK-IN-9 also displays excellent safety and metabolic stability, making it suitable for osteoporosis research. |
| Targets&IC50 | cathepsin K:6.2 nM |
| In vitro | Cathepsin K-IN-9 (Compound 9d) exhibits low cytotoxicity in HEK293T cells at concentrations ranging from 0.001 to 10 μM over 72 hours. At a concentration of 10 μM for 120 minutes, Cathepsin K-IN-9 shows weak inhibition of the five major human CYP isozymes (1A2, 2C9, 2C19, 2D6, 3A4), indicating a low risk of significant metabolic interaction. While there is potential inhibition of the hERG channel at high concentrations (IC 50 = 447 nM), there is no notable cardiac toxicity risk at therapeutic concentrations. Additionally, Cathepsin K-IN-9 is metabolically stable in human, dog, rat, and mouse liver microsomes, with respective remaining amounts of 77.1%, 84.3%, 57.6%, and 69.1% after 30 minutes. |
| Molecular Weight | 575.76 |
| Formula | C35H41N7O |
| Cas No. | 2361420-28-0 |
| Smiles | N#CC=1N=C(NC)C=2C=C(C(=O)NCC3=CC=C(C=C3)C=4C=CC(=CC4)C5CCN(CC5)C6CC6)N(C2N1)CC(C)(C)C |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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