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SKA-121 Sale

目录号 : GC19004

A positive-gating modulator of IKCa1/KCa3.1 channels

SKA-121 Chemical Structure

Cas No.:1820708-73-3

规格 价格 库存 购买数量
500μg 待询 待询
1mg
¥183.00
现货
5mg
¥816.00
现货
10mg
¥1,530.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

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.

Chemical Properties

Cas No. 1820708-73-3 SDF
化学名 5-methyl-naphth[2,1-d]oxazol-2-amine
Canonical SMILES CC1=CC2=C(OC(N)=N2)C3=CC=CC=C13
分子式 C12H10N2O 分子量 198.2
溶解度 DMF: 50 mg/ml,DMSO: 50 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 10 mg/ml 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 5.0454 mL 25.227 mL 50.4541 mL
5 mM 1.0091 mL 5.0454 mL 10.0908 mL
10 mM 0.5045 mL 2.5227 mL 5.0454 mL
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