For research use only. Not for therapeutic Use.
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].
| Catalog Number | I021751 |
| CAS Number | 1957278-93-1 |
| Synonyms | (5S)-5-cyclopropyl-5-[3-[(3S)-4-(3,5-difluorophenyl)-3-methylpiperazin-1-yl]-3-oxopropyl]imidazolidine-2,4-dione |
| Molecular Formula | C20H24F2N4O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H24F2N4O3/c1-12-11-25(6-7-26(12)16-9-14(21)8-15(22)10-16)17(27)4-5-20(13-2-3-13)18(28)23-19(29)24-20/h8-10,12-13H,2-7,11H2,1H3,(H2,23,24,28,29)/t12-,20-/m0/s1 |
| InChIKey | CMLVKUWQFZQPPS-YUNKPMOVSA-N |
| SMILES | CC1CN(CCN1C2=CC(=CC(=C2)F)F)C(=O)CCC3(C(=O)NC(=O)N3)C4CC4 |
| Reference | [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. |
