| Description | Aldumastat (GLPG1972) is a highly potent, specific and orally active inhibitor of ADAMTS-5.Aldumastat is used for the study of osteoarthritis of the knee. |
| In vivo | Aldumastat (GLPG1972;1mg/kg i.v./5mg/kg p.o.)在小鼠、大鼠和狗中显示出良好的药代动力学特性，体内口服生物利用度分别为25%、58%和97%。 |
| Target activity | ADAMTS-5:19 nM, MMP2:1158 nM, ADAMTS-4:156 nM, MMP14:>3198 nM |
| Synonyms | GLPG1972, S201086, G504572 |
| molecular weight | 406.43 |
| Molecular formula | C20H24F2N4O3 |
| CAS | 1957278-93-1 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 80 mg/mL (222.34 mM), Sonication is recommended. |
| References | 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. |