RWJ 50271 is an selective and orally active inhibitor of lymphocyte function-associated antigen-1/intercellular adhesion molecule-1(LFA-1/ICAM-1) interaction with an IC50 of 5.0 μM (HL60 cells). RWJ 50271 inhibits LFA-1/ICAM-1-mediated cell adhesion.
IC50&Target
IC50: 5.0 μM (LFA-1/ICAM-1, HL60 cells)
体外研究
RWJ 50271 inhibits adhesion of peripheral blood lymphocytes to plastic immobilized SICAM-1.
RWJ 50271 inhibits both human and murine NK activity (IC50=5.0 μM) in an LFA-1/ICAM-1-dependent natural killer [NK] cytotoxicity assay.
RWJ 50271 does not inhibit Mac-1/ICAM-1, E-selectidsialyl Lewis X or VLA-4/VCAM-1-mediated cell adhesion up to 20 μM concentrations.
RWJ 50271 does not alter the LFA-1 expression levels on HL60 cells.
RWJ 50271 inhibits adhesion of peripheral blood lymphocytes to plastic immobilized SICAM-1.
RWJ 50271 does not exhibit any toxic activity up to 100 μM concentrations.
体内研究
RWJ 50271 (50 mg/kg; p.o.) is effective in animal model of inflammation.
Animal Model:
Mice, the delayed-type hypersensitivity [DTH] reaction model
Dosage:
50 mg/kg
Administration:
Oral administration
Result:
Significantly reduced foot pad swelling (>50%) 48 h after the challenge.
分子式
C18H17F3N4O2S
分子量
410.41
CAS号
162112-37-0
运输条件
Room temperature in continental US; may vary elsewhere.