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Submit ReviewRA 2 is a potent negative modulator of calcium-activated potassium channels KCa2.3 and KCa3.1 (IC50 values are 2 and 17 nM, respectively), which displays >55-fold selectively for KCa2 and KCa3.1 over other KCa, Kv and Kir channels. In ex vivo porcine coronary endothelium, RA 2 inhibits SKA 31 (Cat. No. 3670)-induced KCa2/KCa3.1 currents and TRAM 34 (Cat. No. 2946)-insensitive KCa2 currents. Reduces heart rate in mice in a KCa3.1-dependent manner.
RA 2 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 414.36 |
公式 | C22H16F2O6 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1867107-62-7 |
InChI Key | XOZKRECPKXTNAK-UHFFFAOYSA-N |
Smiles | OC1=C(C=C(C(OCC2=CC(COC(C3=CC(F)=C(C=C3)O)=O)=CC=C2)=O)C=C1)F |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 41.44 | 100 | |
ethanol | 41.44 | 100 |
以下数据基于产品分子量 414.36。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.41 mL | 12.07 mL | 24.13 mL |
5 mM | 0.48 mL | 2.41 mL | 4.83 mL |
10 mM | 0.24 mL | 1.21 mL | 2.41 mL |
50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
参考文献是支持产品生物活性的出版物。
Olivan-Viguera et al (2015) A novel pan-negative-gating modulator of KCa2/3 channels, fluoro-di-benzoate, RA-2, inhibits endothelium-derived hyperpolarization-type relaxation in coronary artery and produces bradycardia in vivo. Mol.Pharmacol. 338 PMID: 25468883
Olivan-Viguera et al (2016) Vascular reactivity profile of novel KCa3.1-selective positive-gating modulators in the coronary vascular bed. Basic Clin.Pharmacol.Toxicol. 119 184 PMID: 26821335
If you know of a relevant reference for RA 2, please let us know.
关键词: RA 2, RA 2 supplier, RA-2, negative, gating, modulator, KCa, 3.1, 2.3, Ik, SK, calcium, sensitive, activated, potassium, channels, Ca2+-Activated, Potassium, Channels, 7129, Tocris Bioscience
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