Analytical fluorogenic substrates for proteolytic enzymes

Abstract

Fluorogenic substrates for proteolytic enzymes having the formula: ##STR1## or acid salts thereof wherein: R.sub.1 is hydrogen-L, hydrogen-D, benzoyl, benzenesulfonyl, glutaryl, pyroglutamyl, carbobenzoxy, D-serine, or carbobenzoxy-serine; R.sub.2 is hydrogen, phenyl, a straight, branched or cyclic alkyl having 1 to 4 carbons, or propionic acid; R.sub.3 is hydrogen, straight or branched or cyclic alkyl having 1 to 4 carbons, 4-aminobutane, or 3-guanidylpropane; R.sub.4 is methyl, 4-aminobutane, or 3-guanidylpropane; R.sub.5 is a fluorogenic moiety, severable from said compound by a proteolytic enzyme and having different fluorescent property when severed from said compound than when forming part of said compound. The enzymes, when reacting with the substrate, remove the fluorogenic group R.sub.5 producing an increase in its fluorescence. The increase of the fluorescence is an indication of the activity of the enzyme present. Specific enzymes thusly detectable include plasmin, thrombin, the factors X.sub.a, XI.sub.a, & XII.sub.a, kallikrein, trypsin, elastase, urokinase, and cathepsin B.sub.1.

Dependencies are inferred from the claim text.