Pranlukast hemihydrate

SKU: orb1908990

Description

Pranlukast hemihydrate (ONO-1078 hemihydrate) is a selective and potent leukotriene (LT) antagonist with anti-asthmatic activity that inhibits [3H]LTD4 and [3H]LTE4 binding to lung membranes and antagonizes LTC4-induced constriction of guinea-pig airways.Pranlukast hemihydrate is used in the study of asthma. Pranlukast hemihydrate is used in the study of asthma.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	150821-03-7
MW	490.52
Purity	99.28%
Formula	C₂₇H₂₃N₅O₄ 0.5H₂O
SMILES	O=C1C=C(OC=2C(=CC=CC12)NC(=O)C3=CC=C(OCCCCC=4C=CC=CC4)C=C3)C5=NN=NN5.O 0.5H2O
Target	Endogenous Metabolite,Leukotriene Receptor
Solubility	H2O:< 1 mg/mL (insoluble);DMSO:20 mg/mL (40.77 mM)

Bioactivity

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Target IC50	3H-LTC4 to lung membranes:5640 nM (Ki)\|3H-LTE4 to lung membranes:0.63 nM (Ki)\|LTD4:0.99 nM (Ki)
In Vivo	Mice were injected Subcutaneously with different doses of Pranlukast hemihydrate (40, 20, and 10 mM L/kg), AA-861 (20, 10, and 5 mM L/kg), indomethacin (40 mM L/kg), and a control group 30 minutes before LPS injection. Mice treated with AA-861 and Pranlukast hemihydrate showed significantly lower mortality compared to controls. Pretreatment with carrageenan (CAR, 5 mg per mouse, intraperitoneally) sensitized mice to the effects of LPS. Althoug the survival rate of solvent-only treated mice was only 20% at 72 hours after LPS (50 μg per mouse, i.v.) injection, subcutaneous injection of AA-861 (20 mM L/kg) or Pranlukast hemihydrate (40 mM L/kg) significantly increase the survival rate of mice. Read more...
In Vitro	In radioli and binding assays, Pranlukast hemihydrate inhibite the binding of [3H]LTE4, [3H]LTD4, and [3H]LTC4 to lung membranes with Ki Values of 0.63 nM, 0.99 nM, and 5640 nM, respectively Pranlukast hemihydrate inhibited [3H]LTC4 binding competitively the Inhibition of [3H]LTC4 binding by Pranlukast hemihydrate was characterized by competitive antagonism. In functional assays, Pranlukast hemihydrate competitively antagonized LTC4- and LTD4-induced constriction of tracheal and parenchymal and in guinea pigs, with pA2 Values ranging from 7.70 to 10.71. Pranlukast hemihydrate antagonized LTC4-induced constriction of guinea pig tracheal and lung parenchymal ands, even in the presence of an inhibitor o the transition from LTC4 to LTD4. Pranlukast hemihydrate antagonized LTC4-induced tracheal constriction in guinea pigs even in the presence of an inhibitor o the conversion of LTC4 to LTD4 (pA = .78). In addition, Pranlukast hemihydrate significantly reverse the long-term contraction induced by LTD4, but had no significant effect on KCl and BaCl2-induced tracheal contraction in guinea pigs. As a CysLT1 receptor antagonist, Pranlukast hemihydrate (10 μM) inhibits oxygen-glucose deprivation (OGD)-induced nuclear translocation of CysLT1 receptors the effects of Pranlukast hemihydrate on receptor translocation were evaluated in the study wit the 5-lipoxygenase inhibitor Zileuton the results showed that Pranlukast hemihydrate effectively inhibite the nuclear translocation of CysLT1 receptor after 6 hours of OGD, whereas Zileuton did not show such an effect. Read more...

Storage & Handling

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Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Disclaimer	For research use only

Alternative Names

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ONO1078 hemihydrate, ONO-1078 hemihydrate

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Compound Identifiers

PubChem CID

5311184 ↗

Key Properties

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No computed properties available.

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