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MedKoo Cat#: 525716 | Name: Montelukast sodium
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Montelukast is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. Montelukast is a CysLT1 antagonist; it blocks the action of leukotriene D4 (and secondary ligands LTC4 and LTE4) on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it. This reduces the bronchoconstriction otherwise caused by the leukotriene and results in less inflammation.

Chemical Structure

Montelukast sodium
Montelukast sodium
CAS#151767-02-1 (sodium)

Theoretical Analysis

MedKoo Cat#: 525716

Name: Montelukast sodium

CAS#: 151767-02-1 (sodium)

Chemical Formula: C35H35ClNNaO3S

Exact Mass: 0.0000

Molecular Weight: 608.17

Elemental Analysis: C, 69.12; H, 5.80; Cl, 5.83; N, 2.30; Na, 3.78; O, 7.89; S, 5.27

Price and Availability

Size Price Availability Quantity
1g USD 150.00 Ready to ship
5g USD 450.00 Ready to ship
10g USD 850.00 Ready to ship
25g USD 1,350.00 Ready to ship
100g USD 2,950.00 Ready to ship
500g USD 5,850.00 2 weeks
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Related CAS #
151767-02-1 (sodium) 158966-92-8 (free acid)
Synonym
MK-476; MK476; MK 476; Montelukast sodium; trade names Singulair; Montelo-10; Monteflo; Lukotas; Lumona.
IUPAC/Chemical Name
sodium (R,E)-2-(1-(((1-(3-(2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-(2-hydroxypropan-2-yl)phenyl)propyl)thio)methyl)cyclopropyl)acetate
InChi Key
LBFBRXGCXUHRJY-HKHDRNBDSA-M
InChi Code
InChI=1S/C35H36ClNO3S.Na/c1-34(2,40)30-9-4-3-7-25(30)13-17-32(41-23-35(18-19-35)22-33(38)39)27-8-5-6-24(20-27)10-15-29-16-12-26-11-14-28(36)21-31(26)37-29;/h3-12,14-16,20-21,32,40H,13,17-19,22-23H2,1-2H3,(H,38,39);/q;+1/p-1/b15-10+;/t32-;/m1./s1
SMILES Code
CC(C)(C1=CC=CC=C1CC[C@H](C2=CC=CC(=C2)/C=C/C3=NC4=C(C=CC(=C4)Cl)C=C3)SCC5(CC5)CC(=O)[O-])O.[Na+]
Appearance
White to off-white
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in 1:9 EtOH:PBS (pH 7.2), EtOH, DMSO, and DMF
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO or water
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Related CAS# CAS#151767-02-1 (Montelukast sodium salt); CAS#158966-92-8 (Montelukast free acid).
Biological target:
Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1).
In vitro activity:
The SARS-CoV2 is a highly contagious pathogen that causes COVID-19 disease. The in-silico predictions were experimentally validated using vero E6 cells infected with SARS-CoV2 virus. To evaluate the effect of compounds in vitro, Vero E6 cells were seeded in 96 well culture plates. 16 h after seeding the cells were infected with SARS-CoV2 virus at 0.1 MOI for 2 h at 37 °C. Montelukast has been predicted by other groups as well to bind to main protease of SARS-CoV2. Interestingly, many of the predicted molecules viz. capreomycin, celecoxib, mefloquine, montelukast, and nebivolol showed good activity (IC50) against SARS-CoV2. Among the 5 drugs tested mefloquine has the lowest IC50 value at 0.37 uM and montelukast, which was also predicted by others to possess anti-SARS-CoV2 potential has a higher IC50 value of 18.82 uM (Fig. 12, Table 3). The leukotriene inhibitor montelukast is shown to reduce proinflammatory cytokines e.g. TNF-α, IL-6 and IL-1β levels. It has also been suggested that montelukast should be tried as therapeutic option in COVID-19 .The drugs montelukast, celecoxib and nebivolol can cross blood brain barrier , which gives additional advantage to counter neurological manifestations of COVID-19. Comput Struct Biotechnol J. 2021; 19: 1998–2017.Published online 2021 Apr 7. doi: 10.1016/j.csbj.2021.04.014 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8025584/
In vivo activity:
Leukotrienes are involved in neuroinflammation and in the pathological hallmarks of Alzheimer’s disease (AD). The effects of the leukotriene receptor antagonist montelukast (MTK) on hippocampal gene expression in 5xFAD mice, a commonly used transgenic AD mouse model were analyzed. Glial activation and neuroinflammation were identified as the main pathways modulated by MTK. The treatment increased the number of Tmem119+ microglia and downregulated genes related to AD-associated microglia and to lipid droplet-accumulating microglia, suggesting that the MTK treatment targets and modulates microglia phenotypes in the disease model compared to the vehicle. MTK treatment further reduced infiltration of CD8+T-cells into the brain parenchyma.MTK treatment and resulted in improved cognitive functions. The 5xFAD females showed a more severe pathology, and in consequence, MTK treatment had a more pronounced effect in the females compared to the males. The effects on neuroinflammation, i.e., microglia and CD8+ T-cells, as well as the effects on cognitive outcome, were dose-dependent, therefore arguing for the use of higher doses of MTK in AD clinical trials compared to the approved asthma dose. MTK could be a potential drug candidate for AD and provide novel modes of action via modulation of microglia and CD8+ T-cells. Int J Mol Sci. 2021 Mar; 22(5): 2782.Published online 2021 Mar 9. doi: 10.3390/ijms22052782 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7967180/
Solvent mg/mL mM
Solubility
Soluble in DMSO 30.0 49.40
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 608.17 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Kumar S, Singh B, Kumari P, Kumar PV, Agnihotri G, Khan S, Kant Beuria T, Syed GH, Dixit A. Identification of multipotent drugs for COVID-19 therapeutics with the evaluation of their SARS-CoV2 inhibitory activity. Comput Struct Biotechnol J. 2021;19:1998-2017. doi: 10.1016/j.csbj.2021.04.014. Epub 2021 Apr 7. PMID: 33841751; PMCID: PMC8025584. 2.Michael J, Zirknitzer J, Unger MS, Poupardin R, Rieß T, Paiement N, Zerbe H, Hutter-Paier B, Reitsamer H, Aigner L. The Leukotriene Receptor Antagonist Montelukast Attenuates Neuroinflammation and Affects Cognition in Transgenic 5xFAD Mice. Int J Mol Sci. 2021 Mar 9;22(5):2782. doi: 10.3390/ijms22052782. PMID: 33803482; PMCID: PMC7967180.
In vitro protocol:
1. Kumar S, Singh B, Kumari P, Kumar PV, Agnihotri G, Khan S, Kant Beuria T, Syed GH, Dixit A. Identification of multipotent drugs for COVID-19 therapeutics with the evaluation of their SARS-CoV2 inhibitory activity. Comput Struct Biotechnol J. 2021;19:1998-2017. doi: 10.1016/j.csbj.2021.04.014. Epub 2021 Apr 7. PMID: 33841751; PMCID: PMC8025584.
In vivo protocol:
2.Michael J, Zirknitzer J, Unger MS, Poupardin R, Rieß T, Paiement N, Zerbe H, Hutter-Paier B, Reitsamer H, Aigner L. The Leukotriene Receptor Antagonist Montelukast Attenuates Neuroinflammation and Affects Cognition in Transgenic 5xFAD Mice. Int J Mol Sci. 2021 Mar 9;22(5):2782. doi: 10.3390/ijms22052782. PMID: 33803482; PMCID: PMC7967180.
1: Bush A. Montelukast in paediatric asthma: where we are now and what still needs to be done? Paediatr Respir Rev. 2015 Mar;16(2):97-100. doi: 10.1016/j.prrv.2014.10.007. Epub 2014 Dec 12. Review. PubMed PMID: 25499571. 2: Calapai G, Casciaro M, Miroddi M, Calapai F, Navarra M, Gangemi S. Montelukast-induced adverse drug reactions: a review of case reports in the literature. Pharmacology. 2014;94(1-2):60-70. doi: 10.1159/000366164. Epub 2014 Sep 2. Review. PubMed PMID: 25196099. 3: Hon KL, Leung TF, Leung AK. Clinical effectiveness and safety of montelukast in asthma. What are the conclusions from clinical trials and meta-analyses? Drug Des Devel Ther. 2014 Jun 26;8:839-50. doi: 10.2147/DDDT.S39100. eCollection 2014. Review. PubMed PMID: 25061277; PubMed Central PMCID: PMC4079631. 4: Zhang HP, Jia CE, Lv Y, Gibson PG, Wang G. Montelukast for prevention and treatment of asthma exacerbations in adults: Systematic review and meta-analysis. Allergy Asthma Proc. 2014 Jul-Aug;35(4):278-87. doi: 10.2500/aap.2014.35.3745. Review. PubMed PMID: 24992547. 5: Montelukast for Sleep Apnea: A Review of the Clinical Effectiveness, Cost Effectiveness, and Guidelines [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2014 Jan 17. Available from http://www.ncbi.nlm.nih.gov/books/NBK195647/ PubMed PMID: 24741731. 6: Matsuse H, Kohno S. Leukotriene receptor antagonists pranlukast and montelukast for treating asthma. Expert Opin Pharmacother. 2014 Feb;15(3):353-63. doi: 10.1517/14656566.2014.872241. Epub 2013 Dec 19. Review. PubMed PMID: 24350802. 7: Smith TL, Sautter NB. Is montelukast indicated for treatment of chronic rhinosinusitis with polyposis? Laryngoscope. 2014 Aug;124(8):1735-6. doi: 10.1002/lary.24477. Epub 2013 Dec 10. Review. PubMed PMID: 24338615. 8: Yilmaz O, Altintas D, Rondon C, Cingi C, Oghan F. Effectiveness of montelukast in pediatric patients with allergic rhinitis. Int J Pediatr Otorhinolaryngol. 2013 Dec;77(12):1922-4. doi: 10.1016/j.ijporl.2013.10.006. Epub 2013 Oct 19. Review. PubMed PMID: 24210867. 9: Scichilone N, Battaglia S, Benfante A, Bellia V. Safety and efficacy of montelukast as adjunctive therapy for treatment of asthma in elderly patients. Clin Interv Aging. 2013;8:1329-37. doi: 10.2147/CIA.S35977. Epub 2013 Oct 2. Review. PubMed PMID: 24124355; PubMed Central PMCID: PMC3794872. 10: Pacheco Y, Freymond N, Devouassoux G. Impact of montelukast on asthma associated with rhinitis, and other triggers and co-morbidities. J Asthma. 2014 Feb;51(1):1-17. doi: 10.3109/02770903.2013.822081. Epub 2013 Aug 2. Review. PubMed PMID: 23834429. 11: Massingham K, Fox S, Smaldone A. Asthma therapy in pediatric patients: a systematic review of treatment with montelukast versus inhaled corticosteroids. J Pediatr Health Care. 2014 Jan-Feb;28(1):51-62. doi: 10.1016/j.pedhc.2012.11.005. Epub 2013 Jan 9. Review. PubMed PMID: 23312367. 12: Ducharme FM, Noya FJ, Allen-Ramey FC, Maiese EM, Gingras J, Blais L. Clinical effectiveness of inhaled corticosteroids versus montelukast in children with asthma: prescription patterns and patient adherence as key factors. Curr Med Res Opin. 2012 Jan;28(1):111-9. doi: 10.1185/03007995.2011.640668. Epub 2011 Dec 16. Review. PubMed PMID: 22077107. 13: Amlani S, Nadarajah T, McIvor RA. Montelukast for the treatment of asthma in the adult population. Expert Opin Pharmacother. 2011 Sep;12(13):2119-28. doi: 10.1517/14656566.2011.600689. Epub 2011 Jul 22. Review. PubMed PMID: 21777174. 14: Bellecoste V, Devouassoux G, Pacheco Y. [Montelukast in the treatment of mild to moderate persistent asthma]. Rev Mal Respir. 2011 Jun;28(6):706-29. doi: 10.1016/j.rmr.2010.12.008. Epub 2011 May 17. Review. French. PubMed PMID: 21742233. 15: Tintinger GR, Feldman C, Theron AJ, Anderson R. Montelukast: more than a cysteinyl leukotriene receptor antagonist? ScientificWorldJournal. 2010 Dec 14;10:2403-13. doi: 10.1100/tsw.2010.229. Review. PubMed PMID: 21170491. 16: Adsule SM, Misra D. Long term treatment with montelukast and levocetirizine combination in persistent allergic rhinitis: review of recent evidence. J Indian Med Assoc. 2010 Jun;108(6):381-2. Review. PubMed PMID: 21121394. 17: Capsomidis A, Tighe M. Archimedes. Question 2. Is oral montelukast beneficial in treating acute asthma exacerbations in children? Arch Dis Child. 2010 Nov;95(11):948-50. doi: 10.1136/adc.2010.200048. Review. PubMed PMID: 20980280. 18: Castro-Rodriguez JA, Rodrigo GJ. The role of inhaled corticosteroids and montelukast in children with mild-moderate asthma: results of a systematic review with meta-analysis. Arch Dis Child. 2010 May;95(5):365-70. doi: 10.1136/adc.2009.169177. Epub 2009 Nov 27. Review. PubMed PMID: 19946008. 19: Bousquet J, Demoly P, Humbert M. Montelukast in guidelines and beyond. Adv Ther. 2009 Jun;26(6):575-87. doi: 10.1007/s12325-009-0038-1. Epub 2009 Jun 26. Review. PubMed PMID: 19562275. 20: Manalai P, Woo JM, Postolache TT. Suicidality and montelukast. Expert Opin Drug Saf. 2009 May;8(3):273-82. doi: 10.1517/14740330902932688. Review. PubMed PMID: 19505261.

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