Biological Activity
Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 nM.
in vitro
Cyclo(RGDyK) showed higher affinity and selectivity for αVβ3 than αVβ5 and αIIbβ3. Cyclo(RGDyK)-bound micelles (TPM) promoted cell-specific uptake of DiI by B16-F10 cells and HUVECs through integrin-mediated endocytosis compared to Cyclo(RGDyK)-free micelles (NPM).
in vivo
Cyclo(RGDyK) (1 nmol, iv) inhibits the increase in αVβ3 integrin expression in the intima of left stenotic carotid arteries in apoE?/? mice.
target
Target | Value |
αVβ3 integrin | 20 nM |