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Montelukast Sodium LTR antagonist

Name: Montelukast Sodium
Brand: Selleck Chemicals
SKU: S4211
Availability: InStock
Rating: 5 (8 reviews)

Cat.No.S4211

Montelukast Sodium selectively antagonizes leukotriene D₄ (LTD₄) by binding to it so that block the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1. Montelukast improves macroautophagy but not the chaperone-mediated autophagy pathway. Solutions are unstable and should be fresh-prepared.

Chemical Structure

Molecular Weight: 608.17

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Quality Control

Batch: Purity: 99.86%

99.86

Related Targets	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Other LTR Inhibitors	MK-571 sodium salt LY255283 Etalocib

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
HEK293	Function assay	10 mins	Antagonist activity against CysLT1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay, IC50=0.31μM	26985325
HEK293	Function assay	10 mins	Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay, IC50=27μM	26985325
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (164.42 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

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.
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.	5.000mg/ml (8.22mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 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.	0.625mg/ml (1.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.5 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.
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.

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.

Chemical Information, Storage & Stability

Molecular Weight	608.17	Formula	C₃₅H₃₆ClNO₃S.Na	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	151767-02-1	Download SDF		Storage of Stock Solutions	Solutions are unstable. Prepare fresh or purchase small, pre-packaged sizes. Repackage upon receipt.
Synonyms	MK0476			Smiles	CC(C)(C1=CC=CC=C1CCC(C2=CC=CC(=C2)C=CC3=NC4=C(C=CC(=C4)Cl)C=C3)SCC5(CC5)CC(=O)[O-])O.[Na+]

Mechanism of Action

Targets/IC₅₀/Ki	CysLT1
In vitro	Montelukast is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. Montelukast blocks the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus. This reduces the bronchoconstriction otherwise caused by the leukotriene, and results in less inflammation.
In vivo	Montelukast (6 mg/kg, once per day for 20 d) significantly suppresses the increased eosinophils in BAL fluid and lung tissue, and increases IL-5 level in BAL fluid in OVA challenged mice. OVA challenge increases CysLT1 but decreases CysLT2 receptor mRNA expression. Montelukast inhibits the increased CysLT1 but not the reduces CysLT2 expression after OVA challenge.
References	[1] http://en.wikipedia.org/wiki/Montelukast [2] https://pubmed.ncbi.nlm.nih.gov/15456537/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06340984	Not yet recruiting	Acne Vulgaris	South Valley University	June 2024	Phase 3
NCT04351698	Recruiting	Anemia Sickle Cell\|Sleep-Disordered Breathing	Great Ormond Street Hospital for Children NHS Foundation Trust\|Guy''s and St Thomas'' NHS Foundation Trust\|University College London Hospitals\|North Middlesex University Hospital\|King''s College Hospital NHS Trust\|The Whittington Hospital NHS Trust	October 16 2023	Phase 2\|Phase 3
NCT05651750	Unknown status	To Evaluate PSQ as Clinical Tool in the Decision Between Medical and Surgical Treatment for Adenotonsillar Hypertrophy\|To Determine Clinical Response to Montelukast or Nasal Steroids Based on PSQ Results	Assaf-Harofeh Medical Center	November 15 2022	Phase 4
NCT05064631	Recruiting	Respiratory Tract Infections\|Pediatric Respiratory Diseases\|Wheezing	Queen Mary University of London\|Queensland University of Technology	January 12 2022	Phase 2
NCT05710081	Recruiting	Wheezing\|Bronchiolitis\|Asthma in Children	Barts & The London NHS Trust\|University of Aberdeen\|University of Edinburgh\|King''s College London\|University of Southampton\|Menzies School of Health Research	November 30 2021	Phase 3

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