Aldumastat (GLPG1972;S201086) 是一种强效、选择性、口服活性 ADAMTS-5 (IC50=19 nM) 抑制剂，其选择性是 ADAMTS-4 (IC50=156 nM) 的 8 倍。Aldumastat 具有抗代谢活性，用于骨关节炎研究。
Aldumastat (GLPG1972; S201086) is a potent, seletive and orally active ADAMTS-5 (IC50=19 nM) inhibitor, and has 8-fold seletivity over ADAMTS-4 (IC50=156 nM). Aldumastat has anticatabolic activity and is used for osteoarthritis research[1].
GLPG1972 (oral gavage; 5 mg/kg; single dose) displays a favorable PK profile in mice, rats, and dogs. The oral availability (F%) for mice, rats, and dogs are 25%, 58% and 97%, respectively[1].
[1]. Franck Brebion, et al. Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis. J Med Chem. 2021 Mar 25;64(6):2937-2952.
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