BL-1249|cas:18200-13-0|西域试剂

BL-1249,99.88%

产品编号：Bellancom-108596| CAS NO：18200-13-0| 分子式：C₁₇H₁₇N₅| 分子量：291.35

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货号	价格	库存与货期
Bellancom-108596	￥1800.00	杭州北京（现货）
Bellancom-108596	￥2800.00	杭州北京（现货）
Bellancom-108596	￥9800.00	杭州北京（现货）
Bellancom-108596	￥15700.00	杭州北京（现货）

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BL-1249

产品介绍

BL-1249 是一种非甾体抗炎剂 (NSAID) 和钾通道激活剂，可有效激活 K_2P2.1 (TREK-1) 和 K_2P10.1 (TREK-2)，EC₅₀ 值分别为 5.5 μM 和 8.0 μM。BL-1249 在细胞外激活了所有 TREK 亚家族成员，但对其他 K_2P 亚家族没有影响。BL-1249 对膀胱的选择性 (EC₅₀ 为 1.26 μM) 比对血管组织 (EC₅₀ 为 21.0 μM) 更高。

生物活性

BL-1249 is a nonsteroidal anti-inflammatory agent (NSAID) and a potassium channel activator. BL-1249 potently activates K_2P2.1 (TREK-1) and K_2P10.1 (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 K_2P subfamilies. BL-1249 exhibits more selective for the bladder (EC₅₀ of 1.26 μM) than vascular tissue (EC₅₀ of 21.0 μM).

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 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.4323 mL	17.1615 mL	34.3230 mL
5 mM	0.6865 mL	3.4323 mL	6.8646 mL
10 mM	0.3432 mL	1.7161 mL	3.4323 mL

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

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。