BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd < 10 pM). The compound selectively binds to α4β1 (IC50 = 1.8 nM) over various other integrins and results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2].

α9β1:138 nM, α4β1:1.8 nM, α2β1:1053 nM, α4β7:>500 nM

The combination of BIO5192 hydrate (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) produces an additive effect on progenitor mobilization[1]. BIO5192 hydrate (30 mg/kg; s.c.; bid; during days 5 through 14) delays paralysis associated with EAE (experimental autoimmune encephalomyelitis)[2]. BIO5192 hydrate (1 mg/kg, i.v.) has a terminal half-life of 1.1 hours, while doses of 3, 10, and 30 mg/kg s.c. result in half-lives of 1.7, 2.7, and 4.7 hours, respectively. The blood plasma AUC for s.c. administration increases approximately 2.5-fold from 5,460 h*ng/ml for the 3 mg/kg dose to 14,175 h*ng/ml for the 30 mg/kg dose[1]. Animal Model: C57BL/6J x 129Sv/J F1 mice[1].