2. Metabolic Enzyme/Protease
  3. Cathepsin
  4. 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.

Cathepsin K-IN-9

Cathepsin K-IN-9 Chemical Structure

CAS No. : 2361420-28-0

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Cathepsin K-IN-9 Related Antibodies

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Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

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Description

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[1].

IC50 & Target[1]

cathepsin K

6.2 nM (IC50)

In Vitro

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.

Cathepsin K-IN-9 Related Antibodies

Cell Cytotoxicity Assay[1]

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%.
Parmacokinetics
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 %
Molecular Weight

575.75

Formula

C35H41N7O
CAS No.
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
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Cathepsin K-IN-9 Related Classifications

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  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cathepsin K-IN-92361420-28-0CathepsinOsteoporosisCathepsin KCYP1A2CYP2C9CYP2C19CYP2D6CYP3A4hERGInhibitorinhibitorinhibit

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