A Highly Selective Hydantoin Inhibitor of Aggrecanase‑1 and Aggrecanase‑2 with a Low Projected Human Dose
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https://figshare.com/articles/dataset/A_Highly_Selective_Hydantoin_Inhibitor_of_Aggrecanase_1_and_Aggrecanase_2_with_a_Low_Projected_Human_Dose/5154703
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资源简介：
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
