ONO 1078

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Cat.No. 3026 - ONO 1078 | C27H23N5O4 | CAS No. 103177-37-3
Description: Selective CysLT1 antagonist; also TREK2 activator
Alternative Names: Pranlukast
Chemical Name: N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4(4-phenylbutoxy)benzamide
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature (5)

Biological Activity

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.

Compound Libraries

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Technical Data

M. Wt 481.5
Formula C27H23N5O4
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 103177-37-3
PubChem ID 4887
InChI Key NBQKINXMPLXUET-UHFFFAOYSA-N
Smiles O=C2C1=CC=CC(NC(C4=CC=C(OCCCCC5=CC=CC=C5)C=C4)=O)=C1OC(C3=NN=NN3)=C2

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 24.07 50

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.

Select a batch to recalculate based on the batch molecular weight:
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

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References

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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View Related Products by Product Action

View all Leukotriene and Related Receptor Antagonists

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

Citations for ONO 1078

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Literature in this Area

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