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^[1].

CP-69799 (10-fold molar excess; several weeks), a transition-state analogue renin inhibitor with a nitrogen-containing dipeptide isostere, binds tightly to endothiapepsin with a K_i of 0.27 μM, forming extensive hydrogen bonds and van der Waals contacts, and induces subtle domain rearrangements and reduced flap mobility in the enzyme^[1].
CP-69799 inhibits human plasma renin with an IC₅₀ of 0.310 μM at pH 7.0^[1].

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

932.16

C₄₉H₇₃N₉O₉

105116-61-8

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Sali A, et al. High-resolution X-ray diffraction study of the complex between endothiapepsin and an oligopeptide inhibitor: the analysis of the inhibitor binding and description of the rigid body shift in the enzyme. EMBO J. 1989;8(8):2179-2188.  [Content Brief]