Montelukast
- CAS No.
- 158966-92-8
- Chemical Name:
- Montelukast
- Synonyms
- Monteluk;(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;2-[1-[[(1r)-1-[3-[(e)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-[2-(2-hydroxypropan-2-yl)phenyl]propyl]sulfanylmethyl]cyclopropyl]acetic acid;Singular;Montelukas;Montelukast;Montelukastl;Montelukast Acid;Montelukast(Form A);Montelukast free acid
- CBNumber:
- CB7112818
- Molecular Formula:
- C35H36ClNO3S
- Molecular Weight:
- 586.18
- MOL File:
- 158966-92-8.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/7/2 8:55:14
| Melting point | 145-148 °C(Solv: toluene (108-88-3); methanol (67-56-1)) |
|---|---|
| Boiling point | 750.5±60.0 °C(Predicted) |
| Density | 1.272±0.06 g/cm3(Predicted) |
| storage temp. | Store at 2-8°C |
| solubility | DMF: 2 mg/ml,DMSO: 2 mg/ml,Ethanol: insol,PBS (pH 7.2): insol |
| form | A solid |
| pka | 4.76±0.10(Predicted) |
| color | Light yellow to yellow |
| CAS DataBase Reference | 158966-92-8(CAS DataBase Reference) |
| EPA Substance Registry System | Cyclopropaneacetic acid, 1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]- (158966-92-8) |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P264-P280-P302+P352-P305+P351+P338-P332+P313-P337+P313-P362 | |||||||||
| NFPA 704 |
|
Montelukast Chemical Properties,Uses,Production
Uses
cardiostimulant,
Mechanism of action
Montelukast was developed from other weakly antagonistic quinoline derivatives. A number of changes can be made to the structure without the loss of activity. These include changing the double bond between the two aromatic rings to an ether linkage, reducing the quinoline ring, changing the chlorine to a fluorine, and/or exchanging the sulfur for an amide group.
Pharmacokinetics
Montelukast is a high-affinity, selective antagonist of the cysLT1 receptor. It is rapidly absorbed orally, with a bioavailability of 64%. Montelukast is 99% bound to plasma proteins and is extensively metabolized in the liver by CYP3A4 and CYP2C9 to oxidated products. CYP3A4 oxidizes the sulfur and the C-21 benzylic carbon, whereas CYP2C9 is selectively responsible for the methyl hydroxylation.
Side effects
Montelukast did not demonstrate any significant adverse effects greater than placebo in clinical trials; however, because it is metabolized by the cytochrome P450 (CYP450) enzymes, its plasma levels should be monitored when coadministered with CYP450-inducing drugs, such as phenobarbital, rifampin, and phenytoin.
Montelukast Preparation Products And Raw materials
Raw materials
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