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Submit ReviewPMX 205
说明： Potent C5a receptor peptide antagonist
纯度： ≥95% (HPLC)
生物活性 for PMX 205
PMX 205 is a 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. Also improves hindlimb grip strength and slows disease progression in the hSOD1G93A mouse model of amyotrophic lateral sclerosis. Orally active and brain penetrant.
技术数据 for PMX 205
| 分子量 | 839.05 |
| 公式 | C45H62N10O6 |
| 序列 |
XPXWR (Modifications: X-1 = N2-(1-Oxo-3-phenylpropyl)-Orn, X-3 = D-Cha, Lactam bridge: Orn-1 to Arg-5) |
| 储存 | Store at -20°C |
| 纯度 | ≥95% (HPLC) |
| 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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for PMX 205
| 溶解性 | Soluble to 1 mg/ml in water with sonication |
产品说明书 for PMX 205
参考文献 for PMX 205
参考文献是支持产品生物活性的出版物。
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
Lee et al (2017) Pharmacological inhibition of complement C5a-C5a1 receptor signalling ameliorates disease pathology in the hSOD1G93A mouse model of amyotrophic lateral sclerosis. Br.J.Pharmacol. 174 689 PMID: 28128456
Kumar et al (2018) Development and validation of a LC-MS/MS assay for pharmacokinetic studies of complement C5a receptor antagonists PMX53 and PMX205 in mice. Sci.Rep. 8 8101 PMID: 29802264
If you know of a relevant reference for PMX 205, please let us know.
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关键词: PMX 205, PMX 205 supplier, PMX205, potent, c5a, receptor, peptide, antagonist, alzheimer's, disease, alzheimers, antialzheimers, antiinflammatory, Complement, 5196, Tocris Bioscience
2 篇 PMX 205 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PMX 205 的部分引用包括：
Markus et al (2022) Zebrafish fin regeneration involves generic and regeneration-specific osteoblast injury responses. Elife 11 PMID: 35748539
Natarajan et al (2018) Complement Receptor C5aR1 Plays an Evolutionarily Conserved Role in Successful Cardiac Regeneration. Circulation 137 2152 PMID: 29348261
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