PMX 205

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Cat.No. 5196 - PMX 205 | Cyclo[N2-(1-Oxo-3-phenylpropyl)-Orn-Pro-D-Cha-Trp-Arg] | CAS No. 514814-49-4
Description: Potent C5a receptor peptide antagonist
Datasheet
Citations
Literature

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)

Storage Store at -20°C
CAS Number 514814-49-4
PubChem ID 90489023
InChI Key YUIBSMOWXFHTBD-UHFFFAOYSA-N
Smiles NC(=N)NCCCC1NC(=O)C(CC2C=NC3=CC=CC=C23)NC(=O)C(CC2CCCCC2)NC(=O)C2CCCN2C(=O)C(CCCNC1=O)NC(=O)CCC1=CC=CC=C1

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 Data

SolubilitySoluble 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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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


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Keywords: PMX205 potent c5a receptor peptide antagonist alzheimer's disease alzheimers antialzheimers antiinflammatory Complement

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