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.
SKA-121
目录号: GC19004纯度: >99.00%
A positive-gating modulator of IKCa1/KCa3.1 channels
Cas No.: 1820708-73-3
| 规格 | 价格 | 库存 | 数量 | 操作 |
|---|---|---|---|---|
| 5mg | ¥1,956.00 | 现货 | 1 | |
| 10mg | ¥3,681.00 | 现货 | 1 | |
| 25mg | ¥8,701.00 | 现货 | 1 | |
| 10mM (in 1mL DMSO) | ¥871.00 | 现货 | 1 |
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产品描述 Description
实验参考方法 Experimental Reference Method
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). |
References: [1]. Coleman N, et al. New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1. Mol Pharmacol. 2014 Sep;86(3):342-57. |
产品文档 Product Documents
Purity:>99.00%
化学性质Chemical Properties
CAS 号
1820708-73-3
化学名
5-methyl-naphth[2,1-d]oxazol-2-amine
SMILES
CC1=CC2=C(OC(N)=N2)C3=CC=CC=C13
分子式
C12H10N2O
分子量
198.2 g/mol
溶解性
DMF: 50 mg/ml,DMSO: 50 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 10 mg/ml
保存条件
Store at -20°C
General tips
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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
储备液的保存方式和期限：-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。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
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计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度
g/mol