327613-57-0

BIO 5192, is selective, potent inhibitor of integrin α4β1 with an IC50 value of 1.8 ± 0.7 nM. α4β1 regulates the migration of lymphocytes into inflamed tissues, and thus BIO 5192 cna act as an antiinflammatory agent.

bio5192 is a small molecule inhibitor of integrin α4β1 with an ic50 value of 1.8 ± 0.7 nm [1].integrin α4β1 is important in inflammatory processes. in the inflammatory processes, α4β1 regulates the migration of lymphocytes into inflamed tissues [1].in assays using cells expressing α4β7, α9β1, α2β1, and αiibβ3, bio5192 showed high selectivity for α4β1. the affinity of bio5192 for α4β1 was 250- to 1000-fold higher than for α4β7 that shared many ligands the same as α4β1. bio5192 bound even less tightly to α2β1 and αiibβ3. a significant but low level (kd=140 nm) of binding was seen on α9β1 in buffer containing 1 mm mn2+ [1].after 24 h of bio5192 treatment, the lymphocyte count rose about 1.5-fold. half as many cells as when ta-2 was given were released into the circulation following the treatment with bio5192. data showed that bio5192 remained bound to 100% of the α4β1 receptors for 24 h and 50% for 48 h. rats treated with bio5192 at 30 mg/kg, s.c. showed a 1- to 2-day shift when dosed q.d. and a 3-day delay in the onset of disease eae when dosed b.i.d. compared with the control groups. the delay in the onset of eae in the bio5192-treated group was consistent with the finding that bound bio5192 would occupy α4β1 long beyond the point at which the bio5192 was no longer detected in blood [1].

α4β1: 1.8 nM (IC₅₀); α9β1: 138 nM (IC₅₀); α2β1: 1053 nM (IC₅₀); α4β7: >500 nM (IC₅₀)

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[1]. leone dr, giza k, gill a, et al. an assessment of the mechanistic differences between two integrin α4β1 inhibitors, the monoclonal antibody ta-2 and the small molecule bio5192, in rat experimental autoimmune encephalomyelitis[j]. journal of pharmacology and experimental therapeutics, 2003, 305(3): 1150-1162.