| Description | FPS-ZM1 is a high-affinity RAGE specific inhibitor that blocks Aβ binding to the V domain of RAGE. |
| In vitro | FPS-ZM1通过阻断Aβ与RAGE的V区域的结合，抑制了体外表达RAGE细胞中Aβ40和Aβ42引起的细胞应激。它还能阻断其他配体（如S100B、AGE、HMGB1）与RAGE的结合，这些配体被认为在糖尿病、免疫/炎症性疾病以及阿尔茨海默病（AD）[1]模型中通过RAGE介导长期组织损伤的过程中发挥作用。 |
| In vivo | FPS-ZM1对小鼠无毒且能轻松穿过血脑屏障(BBB)。在完全发展了Aβ和淀粉样病理的17月龄APPsw/0小鼠中，通过阻断BBB和大脑中的RAGE作用，有效控制了Aβ介导的脑部疾病进程及相关神经血管和认知功能障碍。此外，FPS-ZM1在17月龄APPsw/0小鼠的大脑中阻断了依赖RAGE的BACE1表达和活性[1]。 |
| Cell experiments | CHO cells are treated for 72 hours with different concentrations of inhibitors ranging from 10 nM to 10 μM. The cellular toxicity was determined using the WST-8 Assay Kit. (Only for Reference) |
| Target activity | RAGE:25 nM. (Ki) |
| molecular weight | 327.85 |
| Molecular formula | C20H22ClNO |
| CAS | 945714-67-0 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 16.67 mg/mL (50.84 mM) |
| References | 1. Deane R, et al. J Clin Invest. 2012, 122(4):1377-1392. 2. He C, Sun S, Zhang Y, et al. The role of irreversible electroporation in promoting M1 macrophage polarization via regulating the HMGB1-RAGE-MAPK axis in pancreatic cancer[J]. OncoImmunology. 2021, 10(1): 1897295. |
| Citations | 1. He C, Sun S, Zhang Y, et al. The role of irreversible electroporation in promoting M1 macrophage polarization via regulating the HMGB1-RAGE-MAPK axis in pancreatic cancer. OncoImmunology. 2021 Mar 11;10(1):1897295. doi: 10.1080/2162402X.2021.1897295. |