Catalog Number: 3496
Chemical Name: (2R)-1-[[2-[(Aminocarbonyl)amino]-4-chlorophenoxy]acetyl]-4-[(4-fluorophenyl)methyl]-2-methylpiperazine
Biological Activity
Potent, 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.
Technical Data
  • M.Wt:
    434.89
  • Formula:
    C21H24ClFN4O3
  • Solubility:
    Soluble to 100 mM in DMSO and to 50 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    217645-70-0
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.
Background References
  1. Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1.
    Liang
    J.Biol.Chem., 2000;275:19000
  2. A chemokine receptor CCR-1 antagonist reduces renal fibrosis after unilateral ureter ligation.
    Anders
    J.Clin.Invest., 2002;109:251
  3. Chemokine receptor CCR1 regulates inflammatory cell infiltration after renal ischemia-reperfusion injury.
    Furuichi et al.
    J.Immunol., 2008;181:8670

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