product name
RAGE 拮抗剂, FPS-ZM1, RAGE Antagonist, FPS-ZM1, is a blood-brain-barrier permeant blocker of RAGE V domain-mediated ligand binding (Ki = 25, 148, & 230 nM, respectively, against Aβ40, HMGB1 & S100B, binding to sRAGE).
质量水平
检测方案
≥98% (HPLC)
形式
semisolid
viscous liquid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white to off-white
溶解性
DMSO: 100 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
O=C(C1=CC=C(Cl)C=C1)N(CC2=CC=CC=C2)C3CCCCC3
一般描述
一种血脑屏障渗透性、无毒的叔酰胺化合物，作为RAGE（晚期糖基化终末产物受体）V结构域介导的配体结合的高亲和力、强效、多模式阻断剂（针对Aβ40、HMGB1和S100B，与sRAGE结合，Ki分别为25、148和230 nM）。阻断RAGE介导的Aβ40和Aβ42流入大脑。还显示出抑制Aβ-RAGE诱导的NF-κB激活和NF-κB-依赖性β-分泌酶转录。据报道，每日对APPsw/0小鼠AD模型（1 mg/kg/d，通过ip）进行治疗，可显著减少皮质和海马体中的硫黄素S阳性淀粉样斑块（减少70%至80%），并将认知能力恢复到非AD小鼠的水平。
生化/生理作用
主要靶标
RAGE
RAGE
可逆性：是
细胞可渗透性：是
靶标Ki：对A&beta分别为25、148和230 nM
包装
用惰性气体包装
警告
毒性：标准处理（A）
重悬
复溶后，等分并冷冻保存（-20°C）。贮备溶液在-20°C下可稳定保存至多6个月。
其他说明
Deane, R., et al. 2012.J. Clin. Invest.122, 1377.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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