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

The combination of BIO5192 hydrate (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization.
BIO5192 hydrate (30 mg/kg; s.c; bid; during days 5 through 14) delays paralysis associated with EAE (experimental autoimmune encephalomyelitis).
BIO5192 hydrate (1 mg/kg, i.v.) shows the terminal half-life is 1.1 hours. BIO5192 hydrate (3, 10, and 30 mg/kg; s.c.) shows half-lives of 1.7, 2.7, and 4.7 hours, respectively. The blood plasma curves show that the AUC for the s.c. route of administration increased about 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.

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