CI 583

• 常用名: CI 583
• 英文名: CI 583
• CAS号: 67254-91-5
• 分子量: 336.14600
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₄H₁₂Cl₂NNaO₃
• 熔点: N/A
• 闪点: N/A

CI 583用途

甲氯苯那酸钠水合物是一种非甾体抗炎剂。甲氯苯那酸水合钠是一种高选择性FTO(脂肪量和肥胖相关)酶抑制剂。甲氯苯那酸钠水合物与FTO结合竞争含m(6)A的核酸。甲氯苯那酸钠水合物是一种非选择性缝隙连接阻断剂。甲氯苯那酸钠水合物抑制hKv2.1和hKv1.1,IC50值分别为56.0和155.9μM[1][2][3][4]。

CI 583名称

• 英文名: sodium meclofenamate monohydrate

CI 583生物活性

• 描述: 甲氯苯那酸钠水合物是一种非甾体抗炎剂。甲氯苯那酸水合钠是一种高选择性FTO(脂肪量和肥胖相关)酶抑制剂。甲氯苯那酸钠水合物与FTO结合竞争含m(6)A的核酸。甲氯苯那酸钠水合物是一种非选择性缝隙连接阻断剂。甲氯苯那酸钠水合物抑制hKv2.1和hKv1.1,IC50值分别为56.0和155.9μM[1][2][3][4]。
• 相关类别:
  研究领域 >> 炎症/免疫
  研究领域 >> 代谢疾病
  研究领域 >> 神经疾病
  信号通路 >> 跨膜转运 >> 钾通道
  信号通路 >> 细胞骨架 >> 间隙连接蛋白
• 靶点实验:

  Human Endogenous Metabolite

• 体外研究: 甲氯苯那酸水合钠(0-100μM,24小时)以剂量反应方式抑制FTO脱甲基[1]。甲氯苯那酸钠水合物抑制环加氧酶,IC50约为1μM,从而抑制前列腺素的产生[2]。甲氯苯那酸钠水合物抑制钙离子载体刺激的人中性粒细胞释放5-HETE和LTB4,并拮抗组织对某些前列腺素的反应[2]。Western Blot分析[1]细胞系：HeLa细胞浓度：0、12.5、25、50、100μM孵育时间：24小时结果：以剂量反应方式抑制FTO去甲基化,并通过靶向FTO提高mRNA中细胞m6A的水平。
• 参考文献:

  [1]. Huang Y, et al. Meclofenamic acid selectively inhibits FTO demethylation of m6A over ALKBH5. Nucleic Acids Res. 2015 Jan;43(1):373-84.

  [2]. Conroy MC, et al. Pharmacology, pharmacokinetics, and therapeutic use of meclofenamate sodium. Clin J Pain. 1991;7 Suppl 1:S44-8.

  [3]. Lee YT, et al. Inhibition of hKv2.1, a major human neuronal voltage-gated K+ channel, by meclofenamic acid. Eur J Pharmacol. 1999 Aug 13;378(3):349-56.

  [4]. Eleftheriou CG, et al. Meclofenamic acid improves the signal to noise ratio for visual responses produced by ectopicexpression of human rod opsin. Mol Vis. 2017 Jun 16;23:334-345. eCollection 2017.

CI 583物理化学性质

• 分子式: C₁₄H₁₂Cl₂NNaO₃
• 分子量: 336.14600
• 精确质量: 335.00900
• PSA: 61.39000
• LogP: 3.41760
• InChIKey: QHJLLDJTVQAFAN-UHFFFAOYSA-M
• SMILES: Cc1ccc(Cl)c(Nc2ccccc2C(=O)[O-])c1Cl.O.[Na+]

CI 583靶点实验

查看更多实验

实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：Fluorescence polarization to screen for inhibitor that competite the binding of FadD2... 来源：Broad Institute 靶标：FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) External Id：2147-01_Inhibitor_SinglePoint_HTS_Activity

实验名称：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfect... 来源：Broad Institute 靶标：N/A External Id：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfected HEK293 cells Inhibition - 7011-01_Antagonist_SinglePoint_HTS_Activity

实验名称：Dicer-mediated maturation of pre-microRNA 来源：Center for Chemical Genomics, University of Michigan 靶标：N/A External Id：TargetID_659_CEMA

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify pos... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_PAM_FLUO8_1536_1X%ACT PRUN

实验名称：Fluorescence polarization-based biochemical high throughput primary assay to identify... 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=Sialate O-acetylesterase; AltName: Full=H-Lse; AltName: Full=Sialic acid-specific 9-O-acetylesterase; Flags: Precursor [Homo sapiens] External Id：SIAE_INH_FP_1536_1X%INH PRUN

实验名称：Absorbance-based primary biochemical high throughput screening assay to identify acti... 来源：The Scripps Research Institute Molecular Screening Center 靶标：caspase-3 preproprotein [Homo sapiens] External Id：PROCASPASE3_ACT_EPIABS_1536_1X%ACT PRUN

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CI 583英文别名

• sodium,2-(2,6-dichloro-3-methylanilino)benzoate,hydrate
• Meclomen
• UNII-94NJ818U2W
• Lenidolor
• Meclodol
• Meclofenamic acid sodium salt monohydrate