Description
A dual antagonist of CCR2 and CCR5 (IC50s = 6.2 and 3.6 nM, respectively, in radioligand binding assays); inhibits chemotaxis induced by the CCR2 ligand MCP-1 in THP-1 cells the CCR5 ligand MIP-1β in isolated peripheral T cells (IC50s = 0.8 and 1.1 nM, respectively); dose-dependently inhibits peritoneal monocyte and macrophage infiltration in an hCCR-2 KI mouse model of thioglycolate-induced peritonitis, with 54% inhibition at 50 mg/kg twice per day
Formal name: N-[(1R,2S,5R)-5-[(1,1-dimethylethyl)amino]-2-[(3S)-3-[[7-(1,1-dimethylethyl)pyrazolo[1,5-a]-1,3,5-triazin-4-yl]amino]-2-oxo-1-pyrrolidinyl]cyclohexyl]-acetamide
Synonyms:
Molecular weight: 484.6
CAS: 1286279-29-5
Purity: ≥98%
Formulation: A crystalline solid
