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.
(Modifications: X-1 = N2-(1-Oxo-3-phenylpropyl)-Orn, X-3 = D-Cha, Lactam bridge: Orn-1 to Arg-5)
|Storage||Store at -20°C|
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.
|Solubility||Soluble to 1 mg/ml in water with sonication|
Preparing Stock Solutions
The following data is based on the product molecular weight 839.05. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.19 mL||5.96 mL||11.92 mL|
|5 mM||0.24 mL||1.19 mL||2.38 mL|
|10 mM||0.12 mL||0.6 mL||1.19 mL|
|50 mM||0.02 mL||0.12 mL||0.24 mL|
References are publications that support the products' biological activity.
March et al (2004) Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activity. Mol.Pharmacol. 65 868 PMID: 15044616
Fonseca et al (2009) Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's disease. J.Immunol. 183 1375 PMID: 19561098
Jain et al (2013) The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10. Br.J.Pharmacol. 168 488 PMID: 22924972
If you know of a relevant reference for PMX 205, please let us know.
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Keywords: PMX 205, supplier, PMX205, potent, c5a, receptor, peptide, antagonist, alzheimer's, disease, alzheimers, antialzheimers, antiinflammatory, Complement, Complement, Tocris Bioscience
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Literature in this Area
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