CAY10614

• 常用名: CAY10614
• 英文名: CAY10614
• CAS号: 1202208-36-3
• 分子量: 755.979
• 密度: N/A
• 沸点: N/A
• 分子式: C₄₂H₇₈INO₂
• 熔点: N/A
• 闪点: N/A

CAY10614用途

CAY10614是一种有效的TLR4拮抗剂。CAY10614抑制脂质A诱导的TLR4激活,IC50为1.675μM。CAY10614可提高致死性内毒素休克模型小鼠的存活率[1][2]。

CAY10614名称

• 中文名: N-环戊基-N,N-二甲基-3,4-双(十四烷基氧基)-苯甲铵碘化物
• 英文名: cyclopentyl-[[3,4-di(tetradecoxy)phenyl]methyl]-dimethylazanium,iodide

CAY10614生物活性

• 描述: CAY10614是一种有效的TLR4拮抗剂。CAY10614抑制脂质A诱导的TLR4激活,IC50为1.675μM。CAY10614可提高致死性内毒素休克模型小鼠的存活率[1][2]。
• 相关类别:
  信号通路 >> 免疫及炎症 >> Toll样受体(TLR)
  研究领域 >> 神经疾病
• 靶点实验:

  TLR4:1.675 μM (IC50, in HEK293 cells)

• 体外研究: CAY10614(化合物7)(1-10μM)以浓度依赖性方式抑制HEK293细胞中脂质A诱导的磷酸酶活性增加[1]。CAY10614(0.5μM)抑制LPS诱导的体外培养(DIV)神经元[Ca2+]cyt的增加[2]。
• 体内研究: CAY10614(化合物7)(10 mg/kg；i、 p.LPS前30分钟)显著提高腹腔注射LPS(20 mg/kg)小鼠的存活率[1]。动物模型：C57BL/6J雄性小鼠(9周)腹腔注射20mg/kg LPS[1]剂量：10mg/kg给药：LPS前30min腹腔注射结果：小鼠存活率从0%提高到67%。
• 参考文献:

  [1]. Piazza M, et, al. Glycolipids and benzylammonium lipids as novel antisepsis agents: synthesis and biological characterization. J Med Chem. 2009 Feb 26;52(4):1209-13.

  [2]. Rodríguez MC, et, al. Aging and amyloid β oligomers enhance TLR4 expression, LPS-induced Ca 2+ responses, and neuron cell death in cultured rat hippocampal neurons. J Neuroinflammation. 2017 Jan 31;14(1):24.

CAY10614物理化学性质

• 分子式: C₄₂H₇₈INO₂
• 分子量: 755.979
• 精确质量: 755.507690
• PSA: 18.46000
• LogP: 10.36940
• InChIKey: UXOPVNPWTUWUEA-UHFFFAOYSA-M
• SMILES: CCCCCCCCCCCCCCOc1ccc(C[N+](C)(C)C2CCCC2)cc1OCCCCCCCCCCCCCC.[I-]

CAY10614靶点实验

查看更多实验

实验名称：Inhibition of calf recombinant intestinal alkaline phosphatase at 10 uM 来源：ChEMBL 靶标：Intestinal-type alkaline phosphatase External Id：CHEMBL996833

实验名称：Inhibition of lipid A-induced TLR4 activation in HEK-Blue-4 cells assessed as inhibit... 来源：ChEMBL 靶标：N/A External Id：CHEMBL996832

实验名称：Inhibition of intestinal alkaline phosphatase in lipid A-stimulated HEK-Blue-4 cells ... 来源：ChEMBL 靶标：Intestinal-type alkaline phosphatase External Id：CHEMBL996834

实验名称：Inhibition of TNF-alpha-induced alkaline phosphatase activity in HEK-Blue-4 cells at ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL996840

实验名称：Antisepsis activity in LPS-induced C57BL/6J mouse lethal endotoxin shock model assess... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL996837

实验名称：Cytotoxicity against HEK-Blue-4 cells assessed as diminution of cell viability by Cel... 来源：ChEMBL 靶标：N/A External Id：CHEMBL996836

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CAY10614英文别名

• Benzenemethanaminium, N-cyclopentyl-N,N-dimethyl-3,4-bis(tetradecyloxy)-, iodide (1:1)
• N-[3,4-Bis(tetradecyloxy)benzyl]-N,N-dimethylcyclopentanaminium iodide