| Description | PMX 205 acetate is an antagonist of complement C5a receptor (C5aR; CD88). |
| In vitro | PMX 205（PMX205）组的活性范围在0.09893至0.2465之间，EP54组在0.02724至0.1748之间，Tamoxifen组的值在0.09880至0.2464之间。在48小时孵化时间的培养板中，仅PMX 205和Tamoxifen两组显示出显著的结果，其值分别在0.04987至0.3273和0.5777至0.8551之间。至于72小时培养板，仅PMX 205（拮抗剂组）展现显著效果，活性值记录在0.02136至0.5322[1]之间。 |
| In vivo | Tg2576小鼠在12至15个月龄期间以20 μg/mL的PMX 205 (PMX205)含药饮水（n=17）进行治疗，在此时段，这些动物的淀粉样蛋白沉积迅速累积。未经治疗的Tg2576动物作为对照组（n=11）。治疗3个月后，使用PMX 205的动物显示出明显较少的纤维斑块负荷（硫黄素反应性）与未治疗动物相比。在3×Tg小鼠中，PMX 205也显著降低超磷酸化tau蛋白（降低69%）[2]。 |
| molecular weight | 899.09 |
| Molecular formula | C47H66N10O8 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/ml (66.73 mM) |
| References | 1. Kosni NN, et al. Expression of complement C5a receptor and the viability of 4T1 tumor cells following agonist-antagonist treatment. J Cancer Res Ther. 2016 Apr-Jun;12(2):590-6. 2. Fonseca MI, et al. Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's disease. J Immunol. 2009 Jul 15;183(2):1375-83. |