CysLT1 antagonist. Downplays contraction of smooth airway muscle, microvascular leakage into airways and eosinophil infiltration. Potential to decrease symptoms of bronchial asthma.
Lynch et al (1999) Characterization of the human leukotriene CysLT1 receptor. Nature 399 789. Heise et al (2000) Characterization of the human cysteinyl leukotriene 2 receptor. J.Biol.Chem. 275 30531. Suzuki et al (2003) Inhibition of human eosinophil activation by a cysteinyl leukotriene receptor antagonist (Pranlukast; ONO-1078). J.Asthma 40 395.
Soluble in DMSO (50 mM), methanol, DMF (~20 mg/ml), water (<1 mg/ml at 25° C), and ethanol (<1 mg/ml at 25° C).
Store at 4° C
741.25° C (Predicted)
~1.4 g/cm3 (Predicted)
n20D 1.68 (Predicted)
CysLT1 Receptor: IC50 = 0.8 nM (human); U-937: IC50 = 1 nM; Binds to the human CysLT1: IC50 = 4-7 nM; Binds to the human CysLT2: IC50 = 3.6 µM; Cruzipain: IC50 = 7 µM (Trypanosoma cruzi)
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