KB130015

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 markedly slows the kinetics of inactivation of Na+ channels. KB130015 activates hERG1 channels (EC50 = 12.2 μM) and large-conductance Ca2+-activated K+ (BKCa) channels formed by hSlo1 (α) subunits in HEK 293 cells. KB130015 has antiarrhythmic properties. KB130015 can be used for the study of cardiovascular disease[1][2][3][4].

Product Specifications

CAS Number

[147030-48-6]

Product Name Alternative

KB015

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Calcium Channel; Potassium Channel; Sodium Channel; Thyroid Hormone Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling; Vitamin D Related/Nuclear Receptor

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/kb130015.html

Purity

98.45

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(COC1=C(C=C(C=C1I)CC2=C(OC3=C2C=CC=C3)C)I)O

Molecular Formula

C18H14I2O4

Molecular Weight

548.11

Precautions

H302, H315, H319, H335

References & Citations

[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.|[4]Gessner G, et al. The amiodarone derivative KB130015 activates hERG1 potassium channels via a novel mechanism. Eur J Pharmacol. 2010 Apr 25;632 (1-3) :52-9.