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Pranlukast Immunology & Inflammation related antagonist

Name: Pranlukast
Brand: Selleck Chemicals
SKU: S1829
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S1829

Pranlukast (ONO-1078,ono-rs-411) is an orally administered, and selective antagonist of the cysteinyl leukotrienes (LT) C(4), LTD(4) and LTE(4), used in the prophylactic treatment of chronic bronchial asthma.

Chemical Structure

Molecular Weight: 481.5

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.82%

99.82

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Chemical Information, Storage & Stability

Molecular Weight	481.5	Formula	C₂₇H₂₃N₅O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	103177-37-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ONO-1078,ono-rs-411			Smiles	C1=CC=C(C=C1)CCCCOC2=CC=C(C=C2)C(=O)NC3=CC=CC4=C3OC(=CC4=O)C5=NNN=N5

Solubility

In vitro
Batch:

DMSO : 11 mg/mL (22.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.200mg/ml (2.49mM)	Taking the 1 mL working solution as an example, add 50 μL of 24 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.600mg/ml (1.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Cysteinyl leukotriene ^[1]
In vitro	Pranlukast inhibits NF-kappa B activation in 1.3% DMSO-differentiated U-937 and Jurkat cells by about 40% & 30%, respectively. This compound and MK-571 inhibit NF-kappa B activation in 1.3% DMSO-differentiated U-937 and Jurkat cells in a dose-related manner. It and MK-571 inhibits LPS-induced IL-6 production in PBMC by about 65% and 15%, respectively. ^[1] This compound or zafirlukast significantly inhibits 10 mM LTD4-evoked 35SO4 output in a concentration-dependent fashion, with maximal inhibitions of 83% at 10 mM Pranlukast and 78% at 10 mM Zafirlukast, and IC50 values of 0.3 mM for Pranlukast and 0.6 mM for Zafirlukast. It (0.5 microM) causes a parallel rightward shift of the LTD4 concentration-response curve with a pKB of 7. This compound or Zafirlukast (5 microM each) significantly suppresses ovalbumin-induced secretion in tracheae from sensitized guinea-pigs by 70% and 65%, respectively. ^[2] It also inhibits NF-kappaB activation induced by phorbol 12-myristate 13-acetate (PMA). This chemical also significantly inhibits LPS-induced MUC2 mRNA expression by reverse transcription-polymerase chain reaction (RT-PCR) analysis in NCI-H292 cells. It also inhibits LPS-induced MUC2 gene expression in HM3-MUC2 cells. ^[3]
In vivo	Pranlukast significantly reduces lesion volume, and increases neuron densities in the cortex and hippocampal CA1 region in the ischemic hemispheres of mice. This compound also remarkably reduces the thickness of a scar wall in the ischemic hemispheres of mice. ^[4]
References	[1] https://pubmed.ncbi.nlm.nih.gov/12801316/ [2] https://pubmed.ncbi.nlm.nih.gov/9647482/ [3] https://pubmed.ncbi.nlm.nih.gov/15475658/ [4] https://pubmed.ncbi.nlm.nih.gov/16051204/

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