Chymase-IN-1

Chymase-IN-1 is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC50 of 29 nM.

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

IC50: 29 nM (chymase)[1]

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.

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