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

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

storage temp. 

-20°C

solubility 

DMSO: 10 mg/ml,Ethanol: 10 mg/ml

form 

A crystalline solid

color 

Off-white to light yellow

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

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

Uses

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].

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. DOI:10.1021/jm001126+
[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. DOI:10.1111/j.1527-3466.2003.tb00117.x
[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. DOI:10.1016/j.ejphar.2006.10.053