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

Names

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

Biological Activity

[Description]:

KB130015 (KB015) is an orally active and potent ThRα and ThRβ (Thyroid Hormone Receptor) inhibitor, with IC50 values of 4.5 and 5.1 μM, respectively. KB130015 has antiarrhythmic properties. KB130015 markedly slows the kinetics of inactivation of Na+ channels. KB130015 opens large-conductance Ca2+-activated K+ channels and relaxes vascular smooth muscle[1][2][3].

[Related Catalog]:

Signaling Pathways >> Others >> Thyroid Hormone Receptor

Research Areas >> Neurological Disease

[Target]

IC50: 4.5 μM (ThRα), 5.1 μM (ThRβ)[1]

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₈H₁₄I₂O₄

[ Molecular Weight ]:
548.11000

[ Exact Mass ]:
547.89800

[ PSA ]:
59.67000

[ LogP ]:
5.00460

Related Compounds

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