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Beschreibung

A structural analog of TAPI-0 (Cat. No. 579050) with similar in vitro efficacy for the inhibition of MMPs and TACE (TNF-alpha convertase, ADAM17). However, TAPI-1 is more stable in serum than TAPI-0. TAPI-1 Blocks the shedding of several cell surface proteins such as TNF-alpha, IL-6 receptor, and p60 and p80 TNF receptors. Inhibits constitutive (IC50 = 8.09 µ,M) and muscarinic receptor-stimulated (IC50 = 3.61 µ,M) sAPPa release in HEK-293 cells expressing muscarinic receptors. Also blocks the TACE-dependent constitutive release of co-transfected APP(695) (IC50 = 920 nM)., A structural analog of TAPI-0 (Cat. No. 579050) with similar in vitro efficacy for the inhibition of MMPs and TACE (TNF-alpha converting enzyme/ADAM17). TAPI-1 also blocks the shedding of several cell surface proteins such as IL-6 receptor, p60 TNF receptor, and p80 TNF receptor. Blocks constitutive (IC50 = 8.09 µ,M) and muscarinic receptor-stimulated (IC50 = 3.61 µ,M) sAAPalpha release in HEK 293 cells expressing M3 muscarinic receptors. A 10 mM (500 µ,g/100 µ,l) solution of TAPI-1 (Cat. No. 579050) in DMSO is also available.