CP-69799

CP-69799 is an azahomostatine-containing oligopeptide transition-state analogue inhibitor with a hog renin IC₅₀ of 6e-9 M, human plasma renin IC₅₀ of 3e-7 M and K_i of 0.310 μM, and endothiapepsin K_i of 0.27 μM. CP-69799 binds endothiapepsin’s active site cleft in extended conformation, fills S4 to S3' pockets, displaces native solvent molecules, induces domain rotation, and reduces thermal mobility of endothiapepsin’s flap and helix regions. CP-69799 acts as a transition-state analogue inhibitor of hog renin and human plasma renin. CP-69799 contains a polar lysine residue at the P2' position, with a nitrogen atom replacing the P1' Cα atom of the hydroxyethylene dipeptide isostere. CP-69799 can be used for the research of hypertension.

• Data Sheet (258 KB)
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