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Submit ReviewSKA 121 is a positive allosteric modulator of KCa3.1 (intermediate-conductance Ca2+-activated potassium) channels (EC50 = 109 nM). Displays 40-fold selectivity for KCa3.1 over KCa2.3, and 200 to 400-fold selectivity over KV and NaV channels. Potentiates bradykinin-induced vasodilation ex vivo. Lowers mean arterial blood pressure in normotensive and hypertensive mice.
分子量 | 198.23 |
公式 | C12H10N2O |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1820708-73-3 |
PubChem ID | 91827362 |
InChI Key | JEGUERWMMMQFJV-UHFFFAOYSA-N |
Smiles | NC(O1)=NC2=C1C3=CC=CC=C3C(C)=C2 |
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 | 19.82 | 100 | |
ethanol | 9.91 | 50 |
以下数据基于产品分子量 198.23。 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 | 5.04 mL | 25.22 mL | 50.45 mL |
5 mM | 1.01 mL | 5.04 mL | 10.09 mL |
10 mM | 0.5 mL | 2.52 mL | 5.04 mL |
50 mM | 0.1 mL | 0.5 mL | 1.01 mL |
参考文献是支持产品生物活性的出版物。
Coleman et al (2014) New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1. Mol.Pharmacol. 86 342 PMID: 24958817
Oliván-Viguera et al (2016) Vascular reactivity profile of novel KCa 3.1-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 SKA 121, please let us know.
关键词: SKA 121, SKA 121 supplier, SKA121, calcium, sensitive, activated, potassium, channel, positive, allosteric, modulators, modulates, kca3.1, intermediate, conductance, SK4, IK, blood, pressure, vasodilation, Ca2+-Activated, Potassium, Channels, 6398, Tocris Bioscience
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