CAS NO: | 147030-48-6 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Cas No. | 147030-48-6 |
别名 | KB015 |
Canonical SMILES | O=C(COC1=C(C=C(CC2=C(C)OC3=C2C=CC=C3)C=C1I)I)O |
分子式 | C18H14I2O4 |
分子量 | 548.1 |
溶解度 | DMSO: 10 mg/ml,Ethanol: 10 mg/ml |
储存条件 | -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | KB-130015 is an antiarrhythmic agent and a derivative of amiodarone .1It inhibits potassium currents induced by acetylcholine or adenosine in isolated guinea pig atrial myocytes (IC50s = 0.82 and 0.57 µM, respectively).2KB-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.3It activates large-conductance calcium-activated potassium (BKCa) channels in HEK293 cells expressing the BKCasubunit Slo1 (EC50= 20.2 μM).4KB-130015 (40 mg/kg) prolongs the duration of electrically stimulated action potentials in guinea pig papillary muscleex vivo.1It is also an antagonist of human thyroid hormone receptor α (TRα) and TRβ (IC50s = 2.2 and 4.1 µM, respectively, in reporter assays). 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 amiodaroneJ. 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 derivativeJ. 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 mechanismEur. 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 muscleEur. J. Pharmacol.555(2-3)185-193(2007) |