MK-0668 is an extremely potent and orally bioavailable antagonist of very late antigen-4 with picomolar, whole blood activity and slow dissociation rates were discovered by incorporating an amino substituent on the proline fragment of the initial lead structure. This level of potency against the unactivated form of VLA-4 was shown to be sufficient to overcome the poor pharmacokinetic profiles typical of this class of VLA-4 antagonists, and sustained activity as measured by receptor occupancy was achieved in preclinical species after orally bioavailable dosing. References: Lin LS, Lanza T, Jewell JP, Liu P, Jones C, Kieczykowski GR, Treonze K, Si Q, Manior S, Koo G, Tong X, Wang J, Schuelke A, Pivnichny J, Wang R, Raab C, Vincent S, Davies P, Maccoss M, Mumford RA, Hagmann WK. Discovery of N-{N-[(3-cyanophenyl)sulfonyl]-4(R)-cyclobutylamino-(L)-prolyl}-4-[(3',5'-dichlor oisonicotinoyl) amino]-(L)-phenylalanine (MK-0668), an extremely potent and orally active antagonist of very late antigen-4. J Med Chem. 2009 Jun 11;52(11):3449-52. doi: 10.1021/jm900257b. PubMed PMID: 19441819.

纯度：≥98%

CAS：865111-04-2