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FPS-ZM1 是一种高亲和力的 RAGE 特异性抑制剂,可阻断 Aβ 与 RAGE 的 V 结构域的结合。
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FPS-ZM1 是一种高亲和力的 RAGE 特异性抑制剂,可阻断 Aβ 与 RAGE 的 V 结构域的结合。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 185 | 现货 | |
5 mg | ¥ 413 | 现货 | |
10 mg | ¥ 622 | 现货 | |
25 mg | ¥ 1,120 | 现货 | |
50 mg | ¥ 1,970 | 现货 | |
100 mg | ¥ 2,970 | 现货 | |
200 mg | ¥ 4,390 | 现货 | |
500 mg | ¥ 6,900 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 455 | 现货 |
产品描述 | FPS-ZM1 is a high-affinity RAGE specific inhibitor that blocks Aβ binding to the V domain of RAGE. |
靶点活性 | RAGE:25 nM. (Ki) |
体外活性 | 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。 |
体内活性 | 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]。 |
激酶实验 | Human sRAGE is immobilized (10 μg/mL) overnight at 4°C in 96-well microtiter plates and blocked with 3% bovine serum albumin. 125I-labeled Aβ40, HMGB1, or S100B at 5 nM in the absence and presence of various concentrations of FPS2 or FPS-ZM1 (10 to 1,000 nM) is added to the wells containing immobilized sRAGE and incubated for 1 hour at room temperature in PBS. Wells are washed with cold PBS to remove unbound radiolabeled ligands, and the radioactivity is analyzed[1]. |
细胞实验 | 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) |
分子量 | 327.85 |
分子式 | C20H22ClNO |
CAS No. | 945714-67-0 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 16.67 mg/mL (50.84 mM) | ||||||||||||||||||||||||||||||
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