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Submit ReviewGI 530159 is a TREK1 and TREK2 channel activator (EC50 = 0.76 μM in Rb efflux assay in TREK1-expressing CHO cells). Exhibits selectivity for TREK1/2 over TRAAK, TASK3 and a range of other potassium channels. Hyperpolarizes membrane potential of dorsal root ganglion neurons and depresses neuronal activity in vitro.
GI 530159 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 | 518.45 |
公式 | C27H20F6N2O2 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 69563-88-8 |
PubChem ID | 94652 |
InChI Key | HHLMWQDRYZAENA-UHFFFAOYSA-N |
Smiles | NC1=CC=C(C=C1)OC2=CC=C(C(C(F)(F)F)(C(F)(F)F)C3=CC=C(C=C3)OC4=CC=C(C=C4)N)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 | 51.84 | 100 | |
ethanol | 25.92 | 50 |
以下数据基于产品分子量 518.45。 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 | 1.93 mL | 9.64 mL | 19.29 mL |
5 mM | 0.39 mL | 1.93 mL | 3.86 mL |
10 mM | 0.19 mL | 0.96 mL | 1.93 mL |
50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
参考文献是支持产品生物活性的出版物。
Loucif et al (2018) GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P) channel opener, reduces rat dorsal root ganglion neuron excitability. Br.J.Pharmacol. 175 2272 PMID: 29150838
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关键词: GI 530159, GI 530159 supplier, GI530159, TREK1, TREK2, channel, activators, activates, K2P2, K2P10, Two-P, Potassium, Channels, 6689, Tocris Bioscience
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