β-Tryptase-IN-1 free base is a selective β-tryptase inhibitor with a K i of 10 nM. β-Tryptase-IN-1 free base binds to the inducible S4 + pocket unique to β-tryptase. β-Tryptase-IN-1 free base can be used for the researches of asthma and chronic obstructive pulmonary disease (COPD) [1].
In Vitro, β-Tryptase-IN-1 (Compound 2) (0.0046-10 μM; 30 min) free base potently inhibits human recombinant β-tryptase with a Ki of 10 nM[1]. β-Tryptase-IN-1 free base shows exquisite selectivity, with no detectable inhibition (IC50 > 100 μM) against factor Xa, thrombin, trypsin, elastase, or chymase[1].
References:
[1]. Liang G, et al. Structure-based library design and the discovery of a potent and selective mast cell β-tryptase inhibitor as an oral therapeutic agent. Bioorg Med Chem Lett. 2012;22(2):1049-1054.
In Vitro, β-Tryptase-IN-1 (Compound 2) (0.0046-10 μM; 30 min) free base potently inhibits human recombinant β-tryptase with a Ki of 10 nM[1]. β-Tryptase-IN-1 free base shows exquisite selectivity, with no detectable inhibition (IC50 > 100 μM) against factor Xa, thrombin, trypsin, elastase, or chymase[1].
References:
[1]. Liang G, et al. Structure-based library design and the discovery of a potent and selective mast cell β-tryptase inhibitor as an oral therapeutic agent. Bioorg Med Chem Lett. 2012;22(2):1049-1054.