Catalog Number: 5196
Biological Activity
Potent C5a receptor peptide antagonist (IC50 = 31 nM). Ameliorates experimentally-induced colon inflammation in mice. Reduces fibrillar amyloid deposits, decreases hyperphosphorylated tau levels and rescues cognitive function in a mouse model of Alzheimer's Disease. Orally active and brain penetrant.
Technical Data
  • M.Wt:
    839.05
  • Formula:
    C45H62N10O6
  • Sequence:
    XPXWR

    (Modifications: X-1 = N2-(1-Oxo-3-phenylpropyl)-Orn, X-3 = D-Cha, Lactam bridge: Orn-1 to Arg-5)

  • Solubility:
    Soluble to 1 mg/ml in water with sonication
  • Storage:
    Store at -20°C
  • CAS No:
    514814-49-4
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. Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activity.
    March et al.
    Mol.Pharmacol., 2004;65:868
  2. Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's disease.
    Fonseca et al.
    J.Immunol., 2009;183:1375
  3. The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10.
    Jain et al.
    Br.J.Pharmacol., 2013;168:488

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