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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.
1. 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. Inhibition of G protein-
3. The amiodarone derivative KB130015 activates hERG1 potassium channels via a novel mechanism. Eur. J. Pharmacol. 632(1-3), 52-59 (2010).
4. The amiodarone derivative 2-