Montelukast
Montelukast is a potent, selective and orally-active antagonist of the cysteinyl leukotriene 1 (CysLT1) receptor, with an IC50 value of 4.9 nM in HEK293 cell membranes expressing human CysLT1 receptors. The CysLT1 receptor is a receptor for cysteinyl leukotrienes (e.g. LTC4, LTD4, and LTE4) which mediate allergic and hypersensitivity reactions in a variety of inflammatory disorders, in particular asthma. Montelukast has been introduced clinically for the treatment of asthma, allergic rhinitis, and exercise-induced bronchoconstriction.
References:
1. Sarau HM, Ames RS, Chambers J, et al. Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor. Molecular Pharmacology, 1999, 56(3): 657-663.
2. Storms W. Update on montelukast and its role in the treatment of asthma, allergic rhinitis and exercise-induced bronchoconstriction. Expert Opinion on Pharmacotherapy, 2007, 8(13): 2173-2187.
3. Eum SY, Maghni K, Hamid Q, et al. Involvement of the cysteinyl-leukotrienes in allergen-induced airway eosinophilia and hyperresponsiveness in the mouse. American Journal of Respiratory Cell and Molecular Biology, 2003, 28(1): 25-32.
| Storage | Store at -20°C |
| M.Wt | 586.18 |
| Cas No. | 158966-92-8 |
| Formula | C35H36ClNO3S |
| Solubility | ≥100mg/mL in DMSO; ≥10mg/mL in Ethanol; Insoluble in H2O |
| Chemical Name | (R,E)-2-(1-(((1-(3-(2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-(2-hydroxypropan-2-yl)phenyl)propyl)thio)methyl)cyclopropyl)acetic acid |
| SDF | Download SDF |
| Canonical SMILES | CC(C)(O)C1=CC=CC=C1CC[C@@H](SCC2(CC2)CC(O)=O)C3=CC=CC(/C=C/C4=CC=C5C(C=C(Cl)C=C5)=N4)=C3 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Animal experiment:[3] | |
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Animal models |
A mouse model of allergic asthma |
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Dosage form |
3 and 10 mg/kg Administered by gavage |
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Applications |
Montelukast inhibited ovalbumin-induced airway hyperresponsiveness and increases in the number of total cells and eosinophils in bronchoalveolar lavage fluid in a mouse model of allergic asthma when administered at doses of 3 and 10 mg/kg. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Sarau HM, Ames RS, Chambers J, et al. Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor. Molecular Pharmacology, 1999, 56(3): 657-663. 2. Storms W. Update on montelukast and its role in the treatment of asthma, allergic rhinitis and exercise-induced bronchoconstriction. Expert Opinion on Pharmacotherapy, 2007, 8(13): 2173-2187. 3. Eum SY, Maghni K, Hamid Q, et al. Involvement of the cysteinyl-leukotrienes in allergen-induced airway eosinophilia and hyperresponsiveness in the mouse. American Journal of Respiratory Cell and Molecular Biology, 2003, 28(1): 25-32. |
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Quality Control & MSDS
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Chemical structure
