BMS-688521,893397-44-9

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BMS-688521

CAS No. : 893397-44-9

MCE 国际站：BMS-688521

产品活性：BMS-688521 是一种高效、具有口服活性的 LFA-1/ICAM 相互作用抑制剂，在粘附试验中 IC₅₀ 为 2.5 nM，在 MLR 试验中 IC₅₀ 为 60 nM。BMS-688521 对小鼠变应性嗜酸性肺炎模型有较好的研究作用。

研究领域：Cytoskeleton

作用靶点：Integrin

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).

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.
BMS-688521 (5 mg/kg; p.o.) treatment shows the C_max, T_max, AUC, F values are 0.32 μM, 1.0 μM, 1.5 μM h, and 50%, respectively.
BMS-688521 (1 mg/kg; i.v.) treatment shows the T_1/2, 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.

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