產(chǎn)品目錄

規(guī)格	1mg 5mg 10mg 25mg
CAS	147030-48-6
別名	N/A
化學(xué)名	N/A
分子式	C18H14I2O4
分子量	548.1
溶解度	DMSO: 10 mg/ml,Ethanol: 10 mg/ml
儲(chǔ)存條件	-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

產(chǎn)品描述：

KB-130015 is an antiarrhythmic agent and a derivative of amiodarone .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 (BKCa) channels in HEK293 cells expressing the BKCa 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).

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)

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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