Senicapoc (ICA-17043) 是有效，选择性的 Gardos 通道 (Ca²⁺ 激活的 K⁺ 通道; KCa3.1) 阻断剂，IC₅₀ 为 11 nM。Senicapoc 阻断来自人红细胞的 Ca²⁺ 诱导的铷通量，IC₅₀ 值为 11 nM， 抑制红细胞脱水的 IC₅₀ 为 30 nM。

Senicapoc (ICA-17043) is a potent and selective Gardos channel (Ca-activated K channel; KCa3.1) blocker with an IC 50 of 11 nM. Senicapoc blocks Ca-induced rubidium flux from human RBCs with an IC 50 value of 11 nM and inhibits RBC dehydration with IC 50 of 30 nM.

Solid

IC50: 11 nM (Gardos channel)

ICA-17043 is shown to block the Gardos channel of mouse (C57 Black) RBCs with an IC50 of 50±6 nM. ICA-17043 blocks this increase in cellular hemoglobin concentration in human RBCs in a concentration-dependent fashion. has not independently confirmed the accuracy of these methods. They are for reference only.

ICA-17043 (10 mg/kg, p.o.) administration produces a significant decrease in Gardos channel activity measured at day 11 and 21 and is associated with a corresponding increase in red cell K content without changes in Na content. ICA-17043 (10 mg/kg, twice a day) induces a significant increase in Hct after 11 days of dosing in the SAD mouse. Senicapoc (30 mg/kg, p.o.) reduces airway hyperresponsiveness, eosinophil numbers in bronchoalveolar lavage taken 48 hours post-allergen challenge, and vascular remodelling in the sheep. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Stocker JW, et al. ICA-17043, a novel Gardos channel blocker, prevents sickled red blood cell dehydration in vitro and in vivo in SAD mice. Blood. 2003 Mar 15;101(6):2412-8.
[2]. Van Der Velden J, et al. K(Ca)3.1 channel-blockade attenuates airway pathophysiology in a sheep model of chronic asthma. PLoS One. 2013 Jun 24;8(6):e66886.

In Vitro: DMSO : 50 mg/mL (154.64 mM; Need ultrasonic)配制储备液