2,6-DIIODO-4-[(2-METHYLBENZOFURAN-3-YL)METHYL]-PHENOXYACETIC ACID

• 常用名: 2,6-DIIODO-4-[(2-METHYLBENZOFURAN-3-YL)METHYL]-PHENOXYACETIC ACID
• 英文名: 2,6-DIIODO-4-[(2-METHYLBENZOFURAN-3-YL)METHYL]-PHENOXYACETIC ACID
• CAS号: 147030-48-6
• 分子量: 548.11000
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₈H₁₄I₂O₄
• 熔点: N/A
• 闪点: N/A

用途

KB130015(KB015)是一种口服有效的ThRα和ThRβ(甲状腺激素受体)抑制剂,IC50值分别为4.5和5.1μM。KB130015具有抗心律失常特性。KB130015显著减缓钠通道失活动力学。KB130015打开大电导钙激活钾通道,松弛血管平滑肌[1][2][3]。

名称

• 英文名: 2-[2,6-diiodo-4-[(2-methyl-1-benzofuran-3-yl)methyl]phenoxy]acetic acid

生物活性

• 描述: KB130015(KB015)是一种口服有效的ThRα和ThRβ(甲状腺激素受体)抑制剂,IC50值分别为4.5和5.1μM。KB130015具有抗心律失常特性。KB130015显著减缓钠通道失活动力学。KB130015打开大电导钙激活钾通道,松弛血管平滑肌[1][2][3]。
• 相关类别:
  信号通路 >> 其他 >> 甲状腺激素受体
  研究领域 >> 神经疾病
• 靶点实验:

  IC50: 4.5 μM (ThRα), 5.1 μM (ThRβ)[1]

• 参考文献:

  [1]. Carlsson B, et al. Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodarone. J Med Chem. 2002 Jan 31;45(3):623-30.

  [2]. Mubagwa K, Macianskiene R, Viappiani S, Gendviliene V, Carlsson B, Brandts B. KB130015, a new amiodarone derivative with multiple effects on cardiac ion channels. Cardiovasc Drug Rev. 2003 Fall;21(3):216-35.

  [3]. Gessner G, et al. The amiodarone derivative 2-methyl-3-(3,5-diiodo-4-carboxymethoxybenzyl)benzofuran (KB130015) opens large-conductance Ca2+-activated K+ channels and relaxes vascular smooth muscle. Eur J Pharmacol. 2007 Jan 26;555(2-3):185-93.

物理化学性质

• 分子式: C₁₈H₁₄I₂O₄
• 分子量: 548.11000
• 精确质量: 547.89800
• PSA: 59.67000
• LogP: 5.00460
• InChIKey: OLIKCJUMYWSDIV-UHFFFAOYSA-N
• SMILES: Cc1oc2ccccc2c1Cc1cc(I)c(OCC(=O)O)c(I)c1

靶点实验

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