| Bioactivity | FK-448 Free base is an effective and specific inhibitor of chymotrypsin, with an IC50 of 720 nM. |
| Target | IC50: 720 nM (Chymotrypsin) |
| Invitro | 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]. |
| Name | FK-448 Free base |
| CAS | 85858-76-0 |
| Formula | C25H30N2O3 |
| Molar Mass | 406.52 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Fujii S, et al. New synthetic inhibitors of chymotrypsin. J Biochem. 1984 Feb;95(2):319-22. [2]. Fujii S, et al. Promoting effect of the new chymotrypsin inhibitor FK-448 on the intestinal absorption of insulin in rats and dogs. J Pharm Pharmacol. 1985 Aug;37(8):545-9. |