BMS 688521 structure
|
Common Name | BMS 688521 | ||
---|---|---|---|---|
CAS Number | 893397-44-9 | Molecular Weight | 536.36600 | |
Density | N/A | Boiling Point | N/A | |
Molecular Formula | C26H19Cl2N5O4 | Melting Point | N/A | |
MSDS | N/A | Flash Point | N/A |
Use of BMS 688521BMS-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 |
---|---|
Synonym | More Synonyms |
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 |
Molecular Formula | C26H19Cl2N5O4 |
---|---|
Molecular Weight | 536.36600 |
Exact Mass | 535.08100 |
PSA | 117.84000 |
LogP | 4.46738 |
unii-n4lds4h73c |
ke-0042 |