tcsc0018187 FK-448 Free base

FK-448 Free base is an effective and specific inhibitor of chymotrypsin, with an IC₅₀ of 720 nM.

IC50 & Target: IC50: 720 nM (Chymotrypsin)^[1]

In Vitro: FK-448 Free base is an effective and specific inhibitor of chymotrypsin, with an IC₅₀ of 720 nM. FK-448 Free base slightly inhibits esterolysis of Trypsin and Thrombin, with IC₅₀s of 780 and 35 μM, respectively, but shows no effects on esterolysis of plasmin, plasma kallikrein or pancreas kallikrein, with IC₅₀s of all >1 mM^[1]. FK-448 moderately inhibits hydrolytic activities of cathepsin G with an IC₅₀ of 15 μM^[2].

In Vivo: FK-448 (20 mg/kg, i.p.) results in a decrease in the blood glucose level, and inhibits the degradation of insulin by pancreatic enzymes in rats. FK-448 (20 mg/kg, p.o.) also decreases the blood glucose level, and increases plasma IRI level in dogs^[2].