BIO-1211 is a peptide inhibitor of α4β1 integrin (IC50 = 0.004 µM).1 It is selective for α4β1 integrin over α4β7 (IC50 = 2 µM), as well as α1β1, α5β1, α6β1, αLβ2, and αIIbβ3 (IC50s = >100 µM for all). BIO-1211 binds to α4β1 (IC50 = 1 nM) and inhibits Jurkat cell adhesion (IC50 = 4 nM). Inhaled administration of BIO-1211 (3 mg/animal) prevents carbachol-induced airway hyperresponsiveness in an ovine model of allergy-induced asthma.
1.Lin, K.c., Ateeq, H.S., Hsiung, S.H., et al.Selective, tight-binding inhibitors of integrin α4β1 that inhibit allergic airway responsesJ. Med. Chem.42(5)920-934(1999)