产品
编 号：F226391
分子式：C17H17N5
分子量：291.35
分子式：C17H17N5
分子量：291.35
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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50mg
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结构图
CAS No: 18200-13-0
产品详情
生物活性：
BL-1249 is a nonsteroidal anti-inflammatory agent (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM).
体内研究：
BL-1249 (1 mg/kg) inhibits isovolumic bladder contractions in vivo. The short duration of the effect of BL-1249 on bladder contraction ( 30 min) is likely due to a fast elimination half-life of the compound after i.v. administration (0.69 h). BL-1249 (1 mg/kg) has little effect on mean arterial blood pressure, an observation again consistent with the in vitro bladder to vascular relaxant selectivity.
体外研究：
BL-1249 produces a concentration-dependent membrane hyperpolarization of cultured human bladder myocytes, assessed as either a reduction in fluorescence of the voltage-sensitive dye bis-(1,2-dibutylbarbituric acid)trimethine oxonol (EC50 of 1.26 μM) or by direct electrophysiological measurement EC50 of 1.49 μM). BL-1249 produced a concentration-dependent hyperpolarization with an EC50 of 21.0 μM in human aortic smooth muscle cells.In in vitro organ bath experiments, BL-1249 produces a concentration-dependent relaxation of 30 mM KCl-induced contractions in rat bladder strips (EC50 of 1.12 μM), yet has no effect on aortic strips up to the highest concentration tested (10 μM). The bladder relaxation produced by BL-1249 is partially blocked by Ba2+ (1 and 10 mM).BL-1249 is a selective agonist of the TREK subfamily when applied extracellularly, having preferential action on K2P2.1(TREK-1) and K2P10.1(TREK-2) over K2P4.1(TRAAK) and establish that its mechanism of action relies on gating at the selectivity filter C-type gate.
BL-1249 is a nonsteroidal anti-inflammatory agent (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM).
体内研究：
BL-1249 (1 mg/kg) inhibits isovolumic bladder contractions in vivo. The short duration of the effect of BL-1249 on bladder contraction ( 30 min) is likely due to a fast elimination half-life of the compound after i.v. administration (0.69 h). BL-1249 (1 mg/kg) has little effect on mean arterial blood pressure, an observation again consistent with the in vitro bladder to vascular relaxant selectivity.
体外研究：
BL-1249 produces a concentration-dependent membrane hyperpolarization of cultured human bladder myocytes, assessed as either a reduction in fluorescence of the voltage-sensitive dye bis-(1,2-dibutylbarbituric acid)trimethine oxonol (EC50 of 1.26 μM) or by direct electrophysiological measurement EC50 of 1.49 μM). BL-1249 produced a concentration-dependent hyperpolarization with an EC50 of 21.0 μM in human aortic smooth muscle cells.In in vitro organ bath experiments, BL-1249 produces a concentration-dependent relaxation of 30 mM KCl-induced contractions in rat bladder strips (EC50 of 1.12 μM), yet has no effect on aortic strips up to the highest concentration tested (10 μM). The bladder relaxation produced by BL-1249 is partially blocked by Ba2+ (1 and 10 mM).BL-1249 is a selective agonist of the TREK subfamily when applied extracellularly, having preferential action on K2P2.1(TREK-1) and K2P10.1(TREK-2) over K2P4.1(TRAAK) and establish that its mechanism of action relies on gating at the selectivity filter C-type gate.
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