An orally bioavailable reversible inhibitor of cathepsin K (Ki(app) = 0.2 nM); selective for cathepsin K over cathepsins B

L-006,235 – 10 mg

Brand:
Cayman
CAS:
294623-49-7
Storage:
-20
UN-No:
Non-Hazardous - /

L-006,235 is an orally bioavailable reversible inhibitor of cathepsin K (Ki(app) = 0.2 nM).{45555} It is selective for cathepsin K over cathepsins B, -L, and -S (Ki(app)s = 1, 6, and 47 µM, respectively). In an in vitro bone resorption assay, L-006,235 inhibits degradation of bovine bone by isolated rabbit osteoclasts (IC50 = 5 nM). L-006,235 (10 mg/kg for 27 days) reduces the loss of lumbar vertebral bone mineral density by 13.3% in ovariectomized rabbits compared to control animals.{45556} It also increases weight bearing, indicating analgesia, in a rat model of osteoarthritis pain when administered at a dose of 100 mg/kg.{45557}  

 

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SKU: 28843 - 10 mg Category:

Description

An orally bioavailable reversible inhibitor of cathepsin K (Ki(app) = 0.2 nM); selective for cathepsin K over cathepsins B, -L, and -S (Ki(app) = 1, 6, and 47 µM, respectively); inhibits degradation of bovine bone by isolated rabbit osteoclasts (IC50 = 5 nM); reduces loss of lumbar vertebral bone mineral density by 13.3% in ovariectomized rabbits at 10 mg/kg for 27 days; increases weight bearing, indicating analgesia, in a rat model of osteoarthritis pain at 100 mg/kg

Formal name: N-[1-[[(cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]-benzamide

Synonyms: 

Molecular weight: 466.6

CAS: 294623-49-7

Purity: ≥98%

Formulation: A solid

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