| CAS | 514814-49-4 |
| Sequence | N2-(1-Oxo-3-phenylpropyl)-Orn-Pro-D-Cha-Trp-Arg-OH(Lactam bridge: Orn-1 to Arg-5) |
| Sequence Single | N2-(1-Oxo-3-phenylpropyl)-Orn-P-D-Cha-WR(Lactam bridge: Orn-1 to Arg-5) |
| Molecular Formula | C45H62N10O6 |
| Molecular Weight | 839.05 |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Description | PMX 205 is a potent complement C5a receptor (C5aR, CD88) antagonist, IC50 = 31 nM. |
| References | 1. Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activity. March et al (2004). Mol.Pharmacol. 65 868 PMID: 15044616 2. Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer’s disease. Fonseca et al (2009). J.Immunol. 183 1375 PMID: 19561098 3. The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10. Jain et al (2013). Br.J.Pharmacol. 168 488 PMID: 22924972 4. Pharmacological inhibition of complement C5a-C5a1 receptor signalling ameliorates disease pathology in the hSOD1G93A mouse model of amyotrophic lateral sclerosis. Lee et al (2017). Br.J.Pharmacol. 174 689 PMID: 28128456 5. Development and validation of a LC-MS/MS assay for pharmacokinetic studies of complement C5a receptor antagonists PMX53 and PMX205 in mice. Kumar et al (2018). Sci.Rep. 8 8101 PMID: 29802264 6. Expression of complement C5a receptor and the viability of 4T1 tumor cells following agonist-antagonist treatment. Kosni NN, et al. J Cancer Res Ther. 2016 Apr-Jun;12(2):590-6. 7. The complement factor C5a contributes to pathology in a rat model of amyotrophic lateral sclerosis. Woodruff TM, et al. J Immunol. 2008 Dec 15;181(12):8727-34. |