BMS-688521

Research use only, not for human use.

BMS-688521 BMS-688521 is an orally active and potent inhibitor of LFA-1/ICAM interaction, a small molecule antagonist of leukocyte function-associated antigen-1 (LFA-1), with potential anti-inflammatory activity.

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.

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).

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 Cmax, Tmax, 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 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.Animal Model: BALB/c female mice, 6-8 week of age (OVA Lung Inflammation in Mice)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.

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Cell Cycle/DNA Damage

Integrin

Integrin

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893397-44-9

536.37

C26H19Cl2N5O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (186.44 mM; Ultrasonic )

O=C1[C@@]2([C@@H](CN(C2)C3=CC=C(C(O)=O)C=N3)C4=CC=C(C#N)C=C4)N(C)C(=O)N1C5=CC(Cl)=CC(Cl)=C5

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(-20℃)

With Ice Pack

≥ 2 years