ONO 1078A CysLT1 antagonist that downplays contraction of smooth airway muscle

ONO 1078 (CAS 103177-37-3)

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Synonym: Pranlukast
Application: A CysLT1 antagonist that downplays contraction of smooth airway muscle
CAS Number: 103177-37-3
Molecular Weight: 481.5
Molecular Formula: C27H23N5O4
* Refer to Certificate of Analysis for lot specific data (including water content).
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CysLT1 antagonist. Downplays contraction of smooth airway muscle, microvascular leakage into airways and eosinophil infiltration. Potential to decrease symptoms of bronchial asthma.


References

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.

Physical State :
Solid
Solubility :
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).
Storage :
Store at 4° C
Melting Point :
236-238° C
Boiling Point :
741.25° C (Predicted)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.68 (Predicted)
IC50 :
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)
Ki Data :
CysLT Receptor: Ki= 0.8 nM (human); Canalicular multispecific organic anion transporter 1: Ki= 41.1 µM (rat)
pK Values :
pKa: 5.33 (Predicted), pKb: 1.4 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
RTECS :
CV5647500
PubChem CID :
115100
Merck Index :
14: 7710
MDL Number :
MFCD00864631
EC Number :
201-616-4
SMILES :
C1=CC=C(C=C1)CCCCOC2=CC=C(C=C2)C(=O)NC3=CC4=C(C=C3)C(=O)C=C(O4)C5=NNN=N5

Download SDS (MSDS)

Certificate of Analysis

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