A Highly Selective Hydantoin Inhibitor of Aggrecanase‑1 and Aggrecanase‑2 with a Low Projected Human Dose
收藏NIAID Data Ecosystem2026-03-10 收录
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Aggrecanase-1 and -2 (ADAMTS-4 and ADAMTS-5) are zinc metalloproteases involved in the degradation of aggrecan in cartilage. Inhibitors could provide a means of altering the progression of osteoarthritis. We report the identification of 7 which had good oral pharmacokinetics in rats and showed efficacy in a rat chemical model of osteoarthritis. The projected human dose required to achieve sustained plasma levels ≥10 times the hADAMTS-5 IC50 is 5 mg q.d.
创建时间：
2017-06-28
