893397-44-9
893397-44-9 structure
- Name: BMS 688521
- Chemical Name: 6-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl]pyridine-3-carboxylic acid
- CAS Number: 893397-44-9
- Molecular Formula: C26H19Cl2N5O4
- Molecular Weight: 536.36600
- Catalog: Signaling Pathways Cytoskeleton Integrin
- Create Date: 2017-07-01 18:56:03
- Modify Date: 2025-09-13 10:43:20
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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[1].
| Name | 6-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl]pyridine-3-carboxylic acid |
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| Synonyms |
unii-n4lds4h73c
ke-0042 |
| 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]. |
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| 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 |
| Molecular Formula | C26H19Cl2N5O4 |
|---|---|
| Molecular Weight | 536.36600 |
| Exact Mass | 535.08100 |
| PSA | 117.84000 |
| LogP | 4.46738 |