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Selective cysteinyl leukotriene receptor 1 (CysLT1) antagonist (IC50 values are ~ 4 - 7 and 3620 nM for CysLT1 and CysLT2 respectively). Inhibits contraction of airway smooth muscle, microvascular leakage into airways and eosinophil infiltration. Can decrease symptoms of bronchial asthma. Also TREK2 activator (pEC50 = 5.8); exhibits selectivity for TREK-2 over other K2P channels.
|Storage||Store at +4°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|
Preparing Stock Solutions
The following data is based on the product molecular weight 481.5. 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|
|0.5 mM||4.15 mL||20.77 mL||41.54 mL|
|2.5 mM||0.83 mL||4.15 mL||8.31 mL|
|5 mM||0.42 mL||2.08 mL||4.15 mL|
|25 mM||0.08 mL||0.42 mL||0.83 mL|
References are publications that support the biological activity of the product.
Lynch et al (1999) Characterization of the human leukotriene CysLT1 receptor. Nature 399 789 PMID: 10391245
Heise et al (2000) Characterization of the human cysteinyl leukotriene 2 receptor. J.Biol.Chem. 275 30531 PMID: 10851239
Suzuki et al (2003) Inhibition of human eosinophil activation by a cysteinyl leukotriene receptor antagonist (Pranlukast; ONO-1078). J.Asthma 40 395 PMID: 12870835
Wright et al (2019) Pranlukast is a novel small molecule activator of the two-pore domain potassium channel TREK2. Biochem.Biophys.Res.Commun. 520 35 PMID: 31564414
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Keywords: ONO 1078, ONO 1078 supplier, Selective, CysLT1, antagonists, Receptors, leukotrienes, eicosanoids, ONO1078, TREK-2, activators, activates, K2P10.1, Pranlukast, Leukotriene, and, Related, Two-P, Potassium, Channels, 3026, Tocris Bioscience
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