C - Chemistry – Metallurgy – 12 – Q
Patent
C - Chemistry, Metallurgy
12
Q
530/5.02, 530/7.
C12Q 1/56 (2006.01) C07K 5/083 (2006.01) C07K 5/087 (2006.01) C07K 5/093 (2006.01) C07K 5/097 (2006.01) C07K 5/103 (2006.01) C12Q 1/37 (2006.01)
Patent
CA 1152494
ABSTRACT Fluorogenic substrates for proteolytic enzymes having the formula: Image or acid salts thereof wherein: R1 is hydrogen-L, hydrogen-D, benzoyl, benzenesulfonyl, glutaryl, pyroglutamyl, carbobenzoxy, D-serine. or carbobenzoxy-serine; R2 is hydrogen, phenyl. a straight, branched or cyclic alkyl having l to 4 carbons, or propionic acid; R3 is hydrogen, straight or branched or cyclic alkyl having I to 4 carbons, 4-aminobutane, or 3-guanidylpropane; R4 is methyl, 4-aminobutane, or 3-guanidylpropane; R5 is a fluorogenic moiety, severable from said compound by a proteo- lytic 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 R5 producing an increase in its fluorescence. The increase of the fluor- escence is an indication of the activity of the enzyme present. Specific enzymes thusly detectable include plasmin, thrombin. the factors Xa, XIa, & XIIa, kallikrein, trypsin, elastase, urokinase, and cathepsin B1.
331214
Gargiulo Robert J.
Hudson Patricia M.
Huseby Rolf M.
Mitchell Gary A.
Pochron Sharon P.
American Hopital Supply Corporation
Macrae & Co.
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