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Pranlukast

SKU: orb1310378

Description

Pranlukast (ONO-1078) is a selective antagonist of the cysteinyl leukotriene receptor 1 (CysLT1), used to inhibit bronchoconstriction in asthma research. It is widely applied in both in vitro binding assays and in vivo models of allergic airway inflammation to study leukotriene-mediated pathways.

Research Area

Cell Biology, Immunology & Inflammation, Metabolism Research, Pharmacology & Drug Discovery, Signal Transduction

Images & Validation

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Pranlukast

Key Properties

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CAS Number103177-37-3
MW481.5
Purity99.98% (May vary between batches)
FormulaC27H23N5O4
SMILESN(C(=O)C1=CC=C(OCCCCC2=CC=CC=C2)C=C1)C3=C4C(C(=O)C=C(O4)C=5NN=NN5)=CC=C3
TargetNF-κB,Endogenous Metabolite,TNF,LTR,Leukotriene Receptor,IL Receptor
SolubilityDMSO:45 mg/mL (93.46 mM);10% DMSO+90% Corn Oil:2 mg/mL (4.15 mM)

Bioactivity

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Target IC50
LTE4:0.63 nM (Ki)|LTC4:5640 nM (Ki)|LTD4:0.99 nM (Ki)
In Vivo
In sensitized guinea pig tracheas, 5 mM of either Pranlukast or Zafirlukast significantly inhibited ovalbumin-induced secretion by 70% and 65%, respectively. These compounds also markedly inhibited 35SO4 release triggered by 10 mM LTD4 in a concentration-dependent manner, with Pranlukast showing a peak inhibition of 83% and Zafirlukast 78% at 10 mM, having IC50 values of 0.3 mM and 0.6 mM, respectively. Pranlukast suppressed the activation of NF-κB in 1.3% DMSO-differentiated U-937 and Jurkat cells, with inhibition rates of 40% and 30%; it also demonstrated a dose-dependent inhibition of NF-κB activation in combination with MK-571. Pranlukast and MK-571 diminished LPS-induced IL-6 production in PBMCs by approximately 65% and 15%. Additionally, Pranlukast inhibited the activation of NF-κB induced by phorbol 12-myristate 13-acetate and significantly reduced LPS-induced MUC2 mRNA expression in NCI-H292 cells, as determined by reverse transcription-polymerase chain reaction. Pranlukast also suppressed the expression of the MUC2 gene in LPS-stimulated HM3-MUC2 cells.
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In Vitro
Pranlukast significantly reduces the volume of injury in the cortical and hippocampal CA1 regions of the ischemic hemisphere in mice and increases neuronal density. Additionally, Pranlukast markedly thins the scar wall in the ischemic hemisphere of mice.
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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CysLTR, Mucin-2, inhibit, Inhibitor, NFκB, NF-κB, ONO 1078, ONO1078, ONO-1078, NFkB, NF-kB, LeukotrieneReceptor, Leukotriene Receptor, IL Receptor, ILReceptor, IL-5, Eosinophil cationic protein, TNF-α, Pranlukast

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Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID
4887 ↗

Key Properties

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No computed properties available.

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Pranlukast (orb1310378)

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50 mg
$ 170.00
250 mg
$ 340.00
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