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BL-1249

CAS No. : 18200-13-0

MCE 站：BL-1249

产品活性：BL-1249 是一种非甾体抗炎药 (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。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Potassium Channel

In Vitro: 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.

In Vivo: 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.

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