FXIIa-IN-6

FXIIa-IN-6 (F38) inhibits recombinant FXIIa activity, with an IC₅₀ of 2 nM^[1].
FXIIa-IN-6 exhibits time-dependent FXIIa inhibition with increased inhibitory potency after preincubation, indicating an irreversible inhibition mechanism^[1].
FXIIa-IN-6 shows high selectivity over homologous serine proteases, including thrombin, PKal, FXa, FXIa, plasmin, tPA, trypsin and chymotrypsin^[1].
LC-MS analysis shows that FXIIa-IN-6 forms a stable covalent adduct with FXIIa, confirming its covalent binding mechanism^[1].
FXIIa-IN-6 significantly prolongs human activated partial thromboplastin time (aPTT), with an EC_1.5X of 11.4 μM, while showing no significant effect on prothrombin time (PT)^[1].
FXIIa-IN-6 (1-20 μM; 12 hours) inhibits IL-6 and IL-1β expression in LPS-stimulated macrophages in a concentration-dependent manner ^[1].
FXIIa-IN-6 (40 μM, 24 hours) in cytotoxicity experiments has no obvious cytotoxicity against RAW264.7 macrophages and maintains more than 80% cell viability in RAW264.7, HEPG2 and HEK-293T cells^[1].
FXIIa-IN-6 irreversibly inhibits FXIIa, with a K_i of 0.51 nM, a k_inact of 0.061 min^-1, and a k_inact/K_i of 0.11740 nM^-1 min^-1[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.