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。
货号:ajcx34496
CAS:1957278-93-1
分子式:C20H24F2N4O3
分子量：406.43
溶解度:DMSO : 100 mg/mL (246.04 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.