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BMS-688521 

Cat. No.: HY-10596
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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.

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BMS-688521 Chemical Structure

BMS-688521 Chemical Structure

CAS No. : 893397-44-9

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10 mM * 1 mL in DMSO USD 679 In-stock
Estimated Time of Arrival: December 31
5 mg USD 575 In-stock
Estimated Time of Arrival: December 31
10 mg USD 980 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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.
Molecular Weight

536.37

Formula

C₂₆H₁₉Cl₂N₅O₄

CAS No.

893397-44-9

SMILES

ClC1=CC(Cl)=CC(N(C(N(C)[[email protected]]23[[email protected]](C4=CC=C(C#N)C=C4)CN(C5=NC=C(C(O)=O)C=C5)C3)=O)C2=O)=C1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

BMS-688521BMS688521BMS 688521IntegrininteractionallergiceosinophiliclunginflammationsplenocytesInhibitorinhibitorinhibit

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