|N-苄基-4-氯-N-环己基苯甲酰胺|CsnPharm

CAS No.: 945714-67-0

N-Benzyl-4-chloro-N-cyclohexylbenzamide Catalog No. CSN17194

Synonyms: FPS-ZM1

FPS-ZM1 is a high-affinity RAGE-specific inhibitor that blocks Aβ binding to the V domain of RAGE with Ki of 25 ± 5 nM in RAGE-transfected CHO cells.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 RAGE

Ki:25±5nM
描述The receptor for advanced glycation end products (RAGE), which belongs to the immunoglobulin superfamily, is a cell-surface receptor for amyloid β-peptide (Aβ) at the blood-brain barrier (BBB), neurons and microglia. FPS-ZM1 is a high-affinity RAGE-specific inhibitor, which prevents Aβ from binding to RAGE in cells and in brain. The inhibitory constant (Ki) of FPS-ZM1 for Aβ/RAGE binding in RAGE-transfected CHO cells is 25 nM. FPS-ZM1 inhibited Aβ-induced generation of thiobarbituric acid–reactive substances with an EC50 value of 28  6 nM in RAGE-CHO cells. The treatment of 50 nM and 500 nM FPS-ZM1 effectively reduced Aβ-induced NF-κB nuclear translocation in RAGE-CHO cells. Stimulation of 1 μM FPS-ZM1 for 24 hours inhibited the excess invasion in 231-RAGE cells caused by RAGE overexpression. In highly metastatic 4175 cells, 24-hour incubation with 1 μM FPS-ZM1 significantly decreased the matrigel invasion. RAGE-mediated Aβ40 influx across the BBB was inhibited by 200 nM FPS-ZM1 by 97% in APP^sw/0 mice at 15 to 17 months old. APP^sw/0 Mice received 1 mg/kg i.p. daily of FPS-ZM1 for 2 months showed significantly decreased Aβ40 and Aβ42 levels by 30%–40% and 60%-80% in cortex and hippocampus respectively. With the same treatment, mRNA and protein levels of different proinflammatory cytokines were reduced by 70%–80% in cortex and hippocampus of the APPsw/0 mice.
作用机制FPS-ZM1 specifically binds to the V domain of RAGE to block Aβ/RAGE interaction, inhibiting Aβ-induced cellular stress in vitro and in vivo.
动物研究
剂量
Rat^[3] (i.p.): min = 1 mg/kg, max = 10 mg/kg

给药途径
i.p.
参考文献

动物研究
剂量	Rat^[3] (i.p.): min = 1 mg/kg, max = 10 mg/kg
给药途径	i.p.

[1] Deane R, Singh I, et al. A multimodal RAGE-specific inhibitor reduces amyloid β-mediated brain disorder in a mouse model of Alzheimer disease. J Clin Invest. 2012 Apr;122(4):1377-92.
[2] Kwak T, Drews-Elger K, et al. Targeting of RAGE-ligand signaling impairs breast cancer cell invasion and metastasis. Oncogene. 2017 Mar;36(11):1559-1572.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0502 mL
- 15.2509 mL
- 30.5018 mL
- 5 mM
- 0.6100 mL
- 3.0502 mL
- 6.1004 mL
- 10 mM
- 0.3050 mL
- 1.5251 mL
- 3.0502 mL

技术信息

CAS号

945714-67-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H22ClNO

运输

蓝冰

分子量

327.85

别名

FPS-ZM1

溶解度

DMSO	65 mg/ml (198.26 mM)
Water	Insoluble

动物实验配方

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N-Benzyl-4-chloro-N-cyclohexylbenzamide Catalog No. CSN17194

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