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BL 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).
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References are publications that support the biological activity of the product.
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.
Keywords: 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
Citations are publications that use Tocris products. Selected citations for BL 1249 include:
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
Do you know of a great paper that uses BL 1249 from Tocris? Please let us know.
Average Rating: 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.
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.