An antiarrhythmic agent
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KB-130015

Item No. 33461

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[2,6-diiodo-4-[(2-methyl-3-benzofuranyl)methyl]phenoxy]-acetic acid
CAS Number
147030-48-6
Molecular Formula
C18H14I2O4
Formula Weight
548.1
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mg/mlEthanol: 10 mg/ml
SMILES
O=C(COC1=C(C=C(CC2=C(C)OC3=C2C=CC=C3)C=C1I)I)O
InChi Code
InChI=1S/C18H14I2O4/c1-10-13(12-4-2-3-5-16(12)24-10)6-11-7-14(19)18(15(20)8-11)23-9-17(21)22/h2-5,7-8H,6,9H2,1H3,(H,21,22)
InChi Key
OLIKCJUMYWSDIV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $185

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    10 mg

    $341

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    25 mg

    $783

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    Product Description

    KB-130015 is an antiarrhythmic agent and a derivative of amiodarone (Item No. 15213).1 It inhibits potassium currents induced by acetylcholine or adenosine in isolated guinea pig atrial myocytes (IC50s = 0.82 and 0.57 µM, respectively).2 KB-130015 activates or inhibits the voltage-gated potassium channel human-ether-a-go-go (hERG), also known as Kv11.1, in HEK293 cells in a voltage-dependent manner.3 It activates large-conductance calcium-activated potassium (KCa1.1/BKCa) channels in HEK293 cells expressing the KCa1.1 subunit Slo1 (EC50 = 20.2 μM).4 KB-130015 (40 mg/kg) prolongs the duration of electrically stimulated action potentials in guinea pig papillary muscle ex vivo.1 It is also an antagonist of human thyroid hormone receptor α (TRα) and TRβ (IC50s = 2.2 and 4.1 µM, respectively, in reporter assays).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Carlsson, B., Singh, B.N., Temciuc, M., et al. Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodarone. J. Med. Chem. 45(3), 623-630 (2002).

    2. Brandts, B., Borchard, R., Macianskiene, R., et al. Inhibition of G protein-coupled and ATP-sensitive potassium currents by 2-methyl-3-(3,5-diiodo-4-carboxymethoxybenzyl)benzofuran (KB130015), an amiodarone derivative. J. Pharmacol. Exp. Ther. 308(1), 134-142 (2004).

    3. Gessner, G., Macianskiene, R., Starkus, J.G., et al. The amiodarone derivative KB130015 activates hERG1 potassium channels via a novel mechanism. Eur. J. Pharmacol. 632(1-3), 52-59 (2010).

    4. Gessner, G., Heller, R., Hoshi, T., 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. 555(2-3), 185-193 (2007).