ADAMTS-5 inhibitor - Compound 12

Based on 20 reference(s) in Google Scholar 80 100 20

Axon 2083

CAS [929634-33-3]

MF C16H11ClF3N3OS3
MW 449.92

Purity: 100%
Soluble in 0.1N NaOH(aq) and DMSO

ADAMTS-5 inhibitor

Description

Inhibitor of ADAMTS-5 (A Disintegrin And Metalloproteinase with ThromboSpondin motifs 5 or aggrecanase-2; IC50 1.1 μM) with >40-fold functional selectivity over ADAMTS-4. ADAMTS-5 is involved in the catabolism of aggrecan and collagen in the articular cartilage matrix during Osteoarthritis (OA).

A.M. Gilbert et al. 5-((1H-Pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5. Bioorg. Med. Chem. Lett. 2007, 17, 1189–1192.

J. Bondeson et al. The regulation of the ADAMTS4 and ADAMTS5 aggrecanases in osteoarthritis: a review. Clin. Exp. Rheumatol. 2008, 26, 139-145.

Selective inhibitor of ADAMTS-5 (aggrecanase-2)

Chemical name

(Z)-5-((5-(4-chlorobenzylthio)-1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one

Parent CAS No.

[929634-33-3]

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ADAMTS-5 inhibitor - Compound 12

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