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Biological Activity:
Novel, oral TACE/MMP inhibitor for rheumatoid arthritis; Apratastat (TMI-005) blocks secretion of soluble TNF-α and down regulates multiple MMPs, which have been implicated in cartilage destruction and bone erosions of RA.
References:
MM Thabet and TWJ Huizinga. Apratastat, a novel TACE/MMP inhibitor for rheumatoid arthritis. Curr. Opin. Investig. Drugs. 2006, 7(11), 1014-1019.
ML Moss et al. Drug Insight: Tumor Necrosis Factor Converting Enzyme as a Pharmaceutical Target for Rheumatoid Arthritis. Nat. Clin. Pract. Rheumatol. 2008, 4(6), 300. [online]
Chemical Name: 4-((4-(2-butynyloxy)phenyl)sulfonyl)-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide
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