Identification | Back Directory | [Name]
2,4-Imidazolidinedione, 5-cyclopropyl-5-[3-[(3S)-4-(3,5-difluorophenyl)-3-methyl-1-piperazinyl]-3-oxopropyl]-, (5S)- | [CAS]
1957278-93-1 | [Synonyms]
GLPG1972 S201086) Aldumastat Aldumastat (GLPG1972 5(R)-Cyclopropyl-5-{3-[4-(3,5-difluoro-phenyl)-3(R)-methyl-piperazin-1-yl]-3-oxo-propyl}-imidazolidine-2,4-dione 2,4-Imidazolidinedione, 5-cyclopropyl-5-[3-[(3S)-4-(3,5-difluorophenyl)-3-methyl-1-piperazinyl]-3-oxopropyl]-, (5S)- | [Molecular Formula]
C20H24F2N4O3 | [MDL Number]
MFCD31690991 | [MOL File]
1957278-93-1.mol | [Molecular Weight]
406.43 |
Chemical Properties | Back Directory | [density ]
1.336±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (246.04 mM; Need ultrasonic) | [form ]
Solid | [pka]
8.79±0.10(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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]. | [IC 50]
ADAMTS-5: 19 nM (IC50); ADAMTS-4: 156 nM (IC50); MMP-2: 1158 nM (IC50); MMP-14: >3198 nM (IC50) | [storage]
Store at -20°C | [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. DOI:10.1021/acs.jmedchem.0c02008 |
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