L-006235

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[1][2].

Product Specifications

CAS Number

[294623-49-7]

Product Name Alternative

L-235

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Cathepsin

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/l-006235.html

Concentration

10mM

Purity

99.93

Solubility

DMSO : 31.25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(NC1(C(NCC#N)=O)CCCCC1)C2=CC=C(C3=CSC(N4CCN(C)CC4)=N3)C=C2

Molecular Formula

C24H30N6O2S

Molecular Weight

466.60

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.|[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.