Aldumastat (Synonyms: GLPG1972; S201086) |
| Catalog No.GC62831 |
알두마스타트(GLPG1972; S201086)는 강력하고 선택적이며 경구 활성인 ADAMTS-5(IC50=19nM) 억제제이며 ADAMTS-4(IC50=156nM)에 비해 8배의 선택성을 갖는다.
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Cas No.: 1957278-93-1
Sample solution is provided at 25 µL, 10mM.
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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].
[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.
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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