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Purity: ≥98%
Montelukast sodium (also known as MK-476; trade names Singulair; Monteflo; Lukotas; Lumona) is a novel, potent, selective CysLT1 (leukotriene receptor) receptor antagonist used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. Montelukast binds to the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes, blocking the action of leukotriene D4 (as well as secondary ligands LTC4 and LTE4) on this receptor. This lessens inflammation and the bronchoconstriction that the leukotriene would have otherwise produced.
| Targets |
CysLT1
|
|---|---|
| ln Vitro |
Montelukast (5 μM; 1 h) prevents cell damage caused by APAP (acetaminophen) (HY-66005)[1].
Montelukast (0.01-10 μM; 30 min) attenuates the plasmin-plasminogen system activation and reduces the 5-oxo-ETE-induced cell migration[3]. Montelukast (10 μM; 18 h) modifies MMP-9 activation[3]. |
| ln Vivo |
Montelukast (3 mg/kg; oral gavage) shields mice's livers from APAP-induced hepatotoxicity[1].
Montelukast (1 mg/kg; miniosmotic pump administration) inhibits the effects of cysteinyl leukotrienes (LT) C4, D4, and E4, which are mediated by the CysLT1 receptor, and lessens the alterations in airway remodeling seen in mice given OVA[2]. Montelukast (1 mg/kg; miniosmotic pump administration) lowers the elevated levels of IL-4 and IL-13 in the BAL fluid of mice treated with OVA[2]. |
| Cell Assay |
Cell Line: Eosinophils
Concentration: 0.01-10 μM
Incubation Time: 30 min
Result: Diminished the 5-oxo-ETE–induced cell migration.
|
| Animal Protocol |
C57BL/6J mice (8-week-old; 22-25 g) are induced acute hepatic injury
3 mg/kg Oral gavage 1 h after saline or APAP administration |
| References |
| Molecular Formula |
C35H35CLNNAO3S
|
|---|---|
| Molecular Weight |
608.17
|
| Exact Mass |
607.19
|
| Elemental Analysis |
C, 69.12; H, 5.80; Cl, 5.83; N, 2.30; Na, 3.78; O, 7.89; S, 5.27
|
| CAS # |
151767-02-1
|
| Related CAS # |
Montelukast; 158966-92-8; Montelukast-d6 sodium; 2673270-26-1; Montelukast dicyclohexylamine; 577953-88-9; Montelukast-d6; 1093746-29-2
|
| Appearance |
White to off-white
|
| SMILES |
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+]
|
| 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
|
| Chemical Name |
sodium;2-[1-[[(1R)-1-[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-[2-(2-hydroxypropan-2-yl)phenyl]propyl]sulfanylmethyl]cyclopropyl]acetate
|
| Synonyms |
Montelukast sodium; MK-476; MK476; MK 476; MK-0476; MK 0476; MK0476; trade names Singulair; Montelo-10; Monteflo; Lukotas; Lumona
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 50~100 mg/mL (82.2~164.4 mM)
Water: ~100 mg/mL Ethanol: ~100 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (2.06 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6443 mL | 8.2214 mL | 16.4428 mL | |
| 5 mM | 0.3289 mL | 1.6443 mL | 3.2886 mL | |
| 10 mM | 0.1644 mL | 0.8221 mL | 1.6443 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04613180 | Active Recruiting |
Drug: Montelukast Sodium Drug: Placebo |
Acute Bronchiolitis | Samarkand State Medical Institute | January 3, 2018 | Phase 4 |
| NCT05894577 | Active Recruiting |
Other: Placebo Drug: Montelukast |
Covid19 | Susanna Naggie, MD | January 27, 2023 | Phase 3 |
| NCT04885530 | Active Recruiting |
Drug: Fluticasone Other: Placebo Drug: Montelukast Drug: Metformin |
Covid19 | Susanna Naggie, MD | June 8, 2021 | Phase 3 |
| NCT05607446 | Recruiting | Drug: TQC3564 tablets Drug: Placebo tablets |
Allergic Rhinitis Drug: T | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. |
September 14, 2022 | Phase 1 |
| NCT04572256 | Recruiting | Drug: Montelukast Drug: Placebo |
ACL Injury Meniscus Tear |
Austin V Stone | February 1, 2021 | Early Phase 1 |
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