Chymase-IN-1 is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC50 of 29 nM.
Chymase-IN-1 (compound 5f) is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC50 of 29 nM. Results demonstrate that Chymase-IN-1 has a chymase Ki value of 36 nM and a Cat G Ki value of 9500 nM[1].
Chymase-IN-1 exhibits low oral bioavailability in rats (F=3%; oral t1/2=1.8 h)[1].
[1]. Greco MN, et al. Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase. J Med Chem. 2007 Apr 19;50(8):1727-30.