Chemical Name: (2R)-1-[[2-[(Aminocarbonyl)amino]-4-chlorophenoxy]acetyl]-4-[(4-fluorophenyl)methyl]-2-methylpiperazine
Biological ActivityPotent, selective non-peptide CCR1 antagonist (Ki = 1 nM for human CCR1). Exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4. Inhibits MIP-α/CCL3-induced intracellular Ca2+ mobilization. Orally active; effectively reduces disease severity in a rat model of multiple sclerosis. Decreases renal fibrosis in a mouse model of obstructive nephropathy.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1.
A chemokine receptor CCR-1 antagonist reduces renal fibrosis after unilateral ureter ligation.
Chemokine receptor CCR1 regulates inflammatory cell infiltration after renal ischemia-reperfusion injury.
Furuichi et al.
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