BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model and it is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction. With an IC50 of 2.5 nM in the adhesion assay and an IC50 of 60 nM in the MLR assay .

BMS-688521 has an IC50 of 78 nM, representing an approximately 30-fold decrease in activity relative to the human T-cell/HUVEC assay data (ICIC50=2.5 nM). BMS-688521 in a mouse specific adhesion assay employed mouse splenocytes and a mouse ICAM-1 expression cell line, b.END3[1].

BMS-688521 (1-10 mg/kg; p.o.; BID for a three-day) is efficacious in a mouse allergic eosinophilic lung inflammation model[1]. BMS-688521 (1 mg/kg; i.v.) treatment shows the T1/2, MRT, CL and Vss values are 1.6 hours, 1.7 hours, 50 mL/mim/kg, and 5.1 L/kg, respectively in BALB/c mice[1]. BMS-688521 (5 mg/kg; p.o.) treatment shows the Cmax, Tmax, AUC, F values are 0.32 μM, 1.0 μM, 1.5 μM h, and 50%, respectively[1].

893397-44-9

C26H19Cl2N5O4

536.37

BMS-688521

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years