1957278-93-1

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].

ADAMTS-5: 19 nM (IC₅₀); ADAMTS-4: 156 nM (IC₅₀); MMP-2: 1158 nM (IC₅₀); MMP-14: >3198 nM (IC₅₀)

Store at -20°C

[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. DOI:10.1021/acs.jmedchem.0c02008