RWJ 50271

• CAT Number: I010919
• CAS Number: 162112-37-0
• Molecular Formula: C18H17F3N4O2S
• Molecular Weight: 410.41
• Purity: ≥95%
• Synonyms: N-(3-hydroxypropyl)-5-methyl-1-[4-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]pyrazole-4-carboxamide
• InChI: InChI=1S/C18H17F3N4O2S/c1-11-14(16(27)22-6-3-7-26)9-23-25(11)17-24-15(10-28-17)12-4-2-5-13(8-12)18(19,20)21/h2,4-5,8-10,26H,3,6-7H2,1H3,(H,22,27)
• InChIKey: HOFGTYCLOKDAES-UHFFFAOYSA-N
• SMILES: CC1=C(C=NN1C2=NC(=CS2)C3=CC(=CC=C3)C(F)(F)F)C(=O)NCCCO

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[1].
RWJ 50271 inhibits adhesion of peripheral blood lymphocytes to plastic immobilized SICAM-1[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[1].
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[1].
RWJ 50271 does not alter the LFA-1 expression levels on HL60 cells[1].
RWJ 50271 inhibits adhesion of peripheral blood lymphocytes to plastic immobilized SICAM-1[1].
RWJ 50271 does not exhibit any toxic activity up to 100 μM concentrations[1].
RWJ 50271 (50 mg/kg; p.o.) is effective in animal model of inflammation[1].

Reference

[1]. Sanfilippo PJ, et al. Novel thiazole based heterocycles as inhibitors of LFA-1/ICAM-1 mediated cell adhesion. J Med Chem. 1995 Mar 31;38(7):1057-9.
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