BMS 688521
Names
Biological Activity
[Description]:
BMS-688521 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 is efficacious in a mouse allergic eosinophilic lung inflammation model[1].
[Related Catalog]:
[In Vitro]
BMS-688521 in a mouse specific adhesion assay employed mouse splenocytes and a mouse ICAM-1 expression cell line, b.END3. 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)[1].
[In Vivo]
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 (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]. 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]. Animal Model: BALB/c female mice, 6-8 week of age (OVA Lung Inflammation in Mice)[1] Dosage: 1, 3, and 10 mg/kg Administration: p.o.; BID for a three-day Result: Significant inhibition of eosinophil accumulation was seen at a dose of 1 mg/kg BID, with dose-dependent inhibition at 3 mg/kg and 10 mg/kg.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C26H19Cl2N5O4
[ Molecular Weight ]:
536.36600
[ Exact Mass ]:
535.08100
[ PSA ]:
117.84000
[ LogP ]:
4.46738