tcsc0018420 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.

IC50 & Target: IC50: 29 nM (chymase)^[1]

In Vitro: 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 K_i value of 36 nM and a Cat G K_i value of 9500 nM^[1].

In Vivo: Chymase-IN-1 exhibits low oral bioavailability in rats (F=3%; oral t_1/2=1.8 h)^[1].