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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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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