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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).
品質等級
化驗
≥98% (HPLC)
形狀
semisolid
viscous liquid
製造商／商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
white to off-white
溶解度
DMSO: 100 mg/mL
運輸包裝
ambient
儲存溫度
2-8°C
SMILES 字串
O=C(C1=CC=C(Cl)C=C1)N(CC2=CC=CC=C2)C3CCCCC3
一般說明
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
包裝
用惰性气体包装
警告
毒性：标准处理（A）
重構
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。
其他說明
Deane, R., et al. 2012.J. Clin. Invest.122, 1377.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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