Aldumastat
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].
Product Specifications
CAS Number
1957278-93-1
Product Name Alternative
GLPG1972; S201086
UNSPSC
12352005
Hazard Statement
H315, H319, H335
Target
ADAMTS
Type
Reference compound
Related Pathways
Metabolic Enzyme/Protease
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Metabolic Disease
Assay Protocol
https://www.medchemexpress.com/aldumastat.html
Purity
99.36
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C(N(CCN1C2=CC(F)=CC(F)=C2)C[C@@H]1C)CC[C@](NC3=O)(C4CC4)C(N3)=O
Molecular Formula
C20H24F2N4O3
Molecular Weight
406.43
Precautions
H315, H319, H335
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
MMP-14; MMP-2
Available Sizes
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