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SKA-121
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
SKA-121图片
包装与价格：
包装价格(元)
500μg电议
1mg电议
5mg电议
10mg电议

产品介绍
SKA-121 是一种选择性 KCa3.1 激活剂。

Kinase experiment:

To fully evaluate the selectivity of the naphthooxazole SKA-121, seven-point concentration-response curves on KCa2.1, KCa2.2, KCa2.3 and KCa3.1 are determined with 250 nM free Ca2+ in the internal solution[1].

Animal experiment:

Mice[1] Twelve-week-old male C57Bl/6J mice are used. For i.v. application, SKA-121 is dissolved at 5 mg/mL in a mixture of 10% CremophorEL and 90% phosphate-buffered saline and then injected at 10 mg/kg into the tail vein (n=8 mice per compound). Another group of mice (n=8) receive SKA-121 orally. At various time points after the injection, blood is collected into EDTA blood sample collection tubes either from the saphenous vein or by cardiac puncture under deep isoflurane anesthesia. After the cardiac puncture, mice are sacrificed by cutting the heart, and then the brain is removed. Individual mice are typically used for three times points (two blood collections from the saphenous vein plus the terminal blood collection).

产品描述 SKA-121 is a positive-gating modulator of intermediate-conductance calcium-activated potassium channels (IKCa1/KCa3.1) with an EC50 value of 109 nM using whole-cell patch-clamp electrophysiology with calcium in the internal solution. It is selective for KCa3.1 over KCa2.1, KCa2.2 and KCa2.3 (EC50s = 8,700, 6,800, and 4,400 nM, respectively). It is also selective over KCa1.1 as well as voltage-gated potassium and sodium channels. SKA-121 (1 uM) potentiates calcium-evoked KCa currents by approximately 7-fold using whole-cell patch-clamp electrophysiology, an effect that can be blocked by the KCa3.1 inhibitor TRAM-34 . It also potentiates calcium-evoked and basal KCa currents. In large porcine coronary arteries ex vivo, SKA-121 potentiates bradykinin-induced endothelium-dependent relaxation (EC50 = 7.9 nM). It also lowers mean arterial blood pressure (MAP) by approximately 20 and 25 mm Hg in normo- and hypertensive mice when used at a dose of 100 mg/kg but has no effect on MAP in KCa3.1 knockout mice.