ONO-5334 is an effective and selective cathepsin K inhibitor (Ki: 0.10 nM, 0.049 nM, and 0.85 nM for human, rabbit, and rat cathepsin K, respectively). ONO-5334 has the potential for the study of osteoporosis.

ONO-5334 has inhibitory effects on human cathepsin S, human cathepsin L, human cathepsin B, porcine calpain Ι and porcine calpain II (Ki: 0.83 nM, 1.7 nM, 32 nM, 82 nM, and 69 nM, respectively). ONO-5334 (0.1-1 μM; 24 hours) inhibits human osteoclast-mediated bone resorption. It effectively decreases the osteoclast-mediated release of CTX from bone slices as a dose-dependent manner[1].

ONO-5334 (p.o.; 0.3-30 mg/kg; 7 consecutive days) at 3 mg/kg or 30 mg/kg obviously reduces CTX (a bone resorption marker) concentration. ONO-5334 (p.o.; 0.12-15 mg/kg; single dose) can dose-dependently decrease PTHrP-induced increase in plasma calcium with significant effect (86% reduction) at 15 mg/kg. It also decreases PTHrP-induced increase in plasma CTX level in TPTX rats by 90% at 15 mg/kg. On day 7, the reduction in serum CTX concentration by ONO-5334 at 3 mg/kg and 30 mg/kg was 62% and 79%, respectively[1].

868273-90-9

C21H34N4O4S

438.58

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years