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Submit ReviewBL 1249 is a K2P2.1 (TREK-1) and K2P10.1 (TREK-2) channel opener (EC50 values are 5.5 μM and 8 μM, respectively). Exhibits selectivity for bladder over vascular tissue in vitro and in vivo (EC50 values are 1.26 and 21.0 μM for cultured bladder and aortic tissues respectively).
分子量 | 291.35 |
公式 | C17H17N5 |
储存 | Store at -20°C |
纯度 | ≥99% (HPLC) |
CAS Number | 18200-13-0 |
PubChem ID | 16078951 |
InChI Key | YYNRZIFBTOUICE-UHFFFAOYSA-N |
Smiles | C1(NC3=CC=CC4=C3CCCC4)=CC=CC=C1C2=NN=NN2 |
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 | |||
1eq. NaOH | 29.14 | 100 | |
DMSO | 29.14 | 100 |
以下数据基于产品分子量 291.35。 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 | 3.43 mL | 17.16 mL | 34.32 mL |
5 mM | 0.69 mL | 3.43 mL | 6.86 mL |
10 mM | 0.34 mL | 1.72 mL | 3.43 mL |
50 mM | 0.07 mL | 0.34 mL | 0.69 mL |
参考文献是支持产品生物活性的出版物。
Tertyshnikova et al (2005) BL-1249 [(5,6,7,8-tetrahydro-naphthalen-1-yl)-[2-(1H-tetrazol-5-yl)-phenyl]-amine]: a putative potassium channel opener with bladder-relaxant properties. J.Pharmacol.Exp.Ther. 313 250 PMID: 15608074
Gonczi et al (2006) Investigation of the role of TASK-2 channels in rat pulmonary arteries; pharmacological and functional studies following RNA interference procedures. Br.J.Pharmacol. 147 496 PMID: 16432512
Pope et al (2018) Protein and chemical determinants of BL-1249 action and selectivity for K2P channels. ACS Chem.Neurosci. 9 3153 PMID: 30089357
If you know of a relevant reference for BL 1249, please let us know.
关键词: BL 1249, BL 1249 supplier, BL1249, potassium, channel, activators, openers, K2p2.1, trek-1, kcnk2, tpkc1, bladder, selective, Two-P, Potassium, Channels, 3797, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 BL 1249 的部分引用包括:
Koichi et al (2019) TREK-1 and TRAAK Are Principal K+ Channels at the Nodes of Ranvier for Rapid Action Potential Conduction on Mammalian Myelinated Afferent Nerves. Neuron 104 960-971.e7 PMID: 31630908
Fernandez-Fernandez et al (2018) Activation of TREK currents by riluzole in three subgroups of cultured mouse nodose ganglion neurons. PLoS One 13 e0199282 PMID: 29928032
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平均评分: 5 (Based on 1 Review.)
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Great potassium channel activator. Was studied on potassium channel expressed on human brain cells. The product performed well under experimental conditions and would purchase again.
The product dissolved in DMSO must be handled carefully as it easily crosses cell membrane.