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KB-130015
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KB-130015图片
CAS NO:147030-48-6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
KB-130015 (KB015) 是一种口服有效的 ThRα 和 ThRβ(甲状腺激素受体)抑制剂,IC50 值分别为 4.5 和 5.1 μM。
Cas No.147030-48-6
别名KB015
Canonical SMILESO=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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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)