MW 499.6 Da, Purity >95%. Stable, selective inhibitor of TNF-α processing (IC₅₀ = ~100 nM). Inhibits TACE (P< 0.01) and other metalloproteases in vivo. Blocks release of TNF-α (IC₅₀ = 50-100 μM), APP (IC₅₀ = 1-8 μM), ACE (IC₅₀ = 10 μM), IL6R (IC₅₀ = 5-10 μM), TNFRI (IC₅₀ = 5-10 μM), TNFRII (IC₅₀ = 25-50 μM), and ObRa (leptin receptor), but not CSF-1 in vivo. Structural analog of TAPI-0.
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