BL-1249 is anonsteroidal anti-inflammatory drug (NSAID)and apotassium channelactivator. BL-1249 potently activatesK_2P2.1 (TREK-1)andK_2P10.1 (TREK-2)withEC₅₀values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates allTREKsubfamily members but has no effect on other K_2Psubfamilies. BL-1249 exhibits more selective for the bladder (EC₅₀of 1.26 μM) than vascular tissue (EC₅₀of 21.0 μM)^[1][2].

EC50: 5.5 μM (TREK-1) and 8.0 μM (TREK-2)^[1]

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 (EC₅₀of 1.26 μM) or by direct electrophysiological measurementEC₅₀of 1.49 μM). BL-1249 produced a concentration-dependent hyperpolarization with anEC₅₀of 21.0 μM in human aortic smooth muscle cells^[1].
In in vitro organ bath experiments, BL-1249 produces a concentration-dependent relaxation of 30 mM KCl-induced contractions in rat bladder strips (EC₅₀of 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)^[1].
BL-1249 is a selective agonist of the TREK subfamily when applied extracellularly, having preferential action on K_2P2.1(TREK-1) and K_2P10.1(TREK-2) over K_2P4.1(TRAAK) and establish that its mechanism of action relies on gating at the selectivity filter C-type gate^[2].

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)^[1].
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^[1].

291.35

Solid

C₁₇H₁₇N₅

18200-13-0

Room temperature in continental US; may vary elsewhere.

DMSO : 50 mg/mL(171.61 mM;ultrasonic and warming and heat to 60℃)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (8.58 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.58 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (8.58 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.58 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。