L-873724是一种有效、可口服、选择性、可逆的非碱性cathepsinK抑制剂，对cathepsinK，cathepsinS，cathepsinL，cathepsinB的IC50值分别为0.2，178，264和5239nM。L-873724抑制兔子cathepsinK的活性，IC50值为0.5nM，同时可抑制骨再吸收
CAS：603139-12-4
分子式：C23H26F3N3O3S
分子量：481.53
纯度：98%
存储：Store at -20°C

Background:

L-873724 is a potent, orally bioavailable, selective and reversible[2] non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively[1]. L-873724 also exhibits an IC50 of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption[2].

L-873724 (Compound 22) is a potent and selective non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also shows IC50s of 95, 1221 and 4807 nM for Ramos cathepsin S, Hep G2 cathepsin L, Hep G2 cathepsin B[1]. L-873724 exhibits an IC50 of 0.5 nM for rabbit cathepsin K[2].

L-873724 is orally bioavailable, non-lysosomotropic, and efficacious in the rhesus monkey bone resorption model[1].

[1]. Li CS, et al. Identification of a potent and selective non-basic cathepsin K inhibitor. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1985-9. [2]. Zhuo Y, et al. Inhibition of bone resorption by the cathepsin K inhibitor odanacatib is fully reversible. Bone. 2014 Oct;67:269-80.