Cathepsin K-IN-9
Cathepsin K-IN-9 is a selective, potent and orally active Cathepsin K inhibitor with an IC50 of 6.2 nM. Cathepsin K-IN-9 has IC50 > 10000 nM for cathepsin B, L, and S, showing over 1600-fold selectivity. Cathepsin K-IN-9 has excellent safety and metabolic stability.Cathepsin K-IN-9 can be used for the research of osteoporosis.
For research use only. We do not sell to patients.
- CAS No.: 2361420-28-0
- Formula: C35H41N7O
- Molecular Weight:575.75
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All Cathepsin Isoforms
More
Biological Activity
|
cathepsin K 6.2 nM (IC50) |
Cathepsin K-IN-9 (Compound 9d) (0.001–10 μM; 72 h) demonstrates low cytotoxicity in HEK293T cells[1].
Cathepsin K-IN-9 (10 μM, 120 min) exhibits weak inhibition against five major human CYP isozymes (1A2, 2C9, 2C19, 2D6, 3A4), with no significant risk of metabolic interactions[1].
Cathepsin K-IN-9 inhibits the hERG channel at high concentrations (IC50 = 447 nM), but shows no significant cardiotoxicity risk at therapeutic concentrations[1].
Cathepsin K-IN-9 exhibits moderate metabolic stability in human, dog, rat, and mouse liver microsomes, with 77.1%, 84.3%, 57.6%, and 69.1% of the compound remaining after 30 minutes, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HEK293T cells
-
Concentration:0.001, 0.004, 0.01, 0.01, 0.1, 0.3, 1.1, 3.3 and 10 μM
-
Incubation Time:72 h
-
Result:Maintained cell vitality at over 70%.
| Species | Dose | Route | AUC | T1/2 | CL_obs | Vss_obs | F |
|---|---|---|---|---|---|---|---|
| Rat | 1 mg/kg | i.v. | 1482 ng·h/mL | 6 h | 10.9 mL/min/kg | 3.7 L/kg | / |
| Rat | 10 mg/kg | p.o. | 4200 ng·h/mL | 5.5 h | / | / | 28.3 % |
Chemical Information
-
CAS No. 2361420-28-0
-
Molecular Weight 575.75
-
Formula C35H41N7O
-
SMILES
CNC1=NC(C#N)=NC2=C1C=C(N2CC(C)(C)C)C(NCC3=CC=C(C=C3)C4=CC=C(C=C4)C5CCN(CC5)C6CC6)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Cathepsin K-IN-9 Related Classifications
HY-179697 Related Classifications
Powered by Bioz