Catalog Number: 4528
Chemical Name: N-1-[(3-4(-Ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)benzeneacetamide
Biological Activity
Potent and selective CXCR3 antagonist; potently inhibits 125I-CXCL10 binding to CXCR3 (pKi = 8.13). Inhibits calcium mobilization in response to CXCL11 and CXCL10 in RBL cells. Exhibits no significant effect on chemotaxis induced by CXCR4 or CCR7. Displays a five-fold greater affinity for CXCR3 than (±)-AMG 487 (Cat. No. 4487).
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 50 mM in DMSO
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
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.
Additional Information
Other Product-Specific Information:
  • This compound is racemic
Background References
  1. Synthesis and structure-activity relationships of 3H-quinazolin-4-ones and 3H-pyrido[2,3-d]pyrimidin-4-ones as CXCR3 receptor antagonists.
    Storelli et al.
    Arch.Pharm., 2007;340:281
  2. Noncompetitive antagonism and inverse agonism as mechanism of action of nonpeptidergic antagonists at primate and rodent CXCR3 chemokine receptors.
    Verzijl et al.
    J.Pharmacol.Exp.Ther., 2008;325:544
  3. Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist.
    Heise et al.
    J.Pharmacol.Exp.Ther., 2005;313:1263
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