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 Ki of 0.310 µM, and endothiapepsin Ki of 0.27 µM. CP-69799 binds endothiapepsins active site cleft in extended conformation, fills S4 to S3 pockets, displaces native solvent molecules, induces domain rotation, and reduces thermal mobility of endothiapepsins 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 Calpha atom of the hydroxyethylene dipeptide isostere. CP-69799 can be used for the research of hypertension[1].
Molekulargewicht:
932.16
CAS Nummer:
[105116-61-8]
Formel:
C49H73N9O9
Target-Kategorie:
Enteropeptidase,Renin
Anwendungsbeschreibung:
MCE Product type: Peptides
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
