107753-78-6
107753-78-6 structure
- Name: Zafirlukast
- Chemical Name: zafirlukast
- CAS Number: 107753-78-6
- Molecular Formula: C31H33N3O6S
- Molecular Weight: 575.675
- Catalog: API Antiallergic Allergic reaction medium blocker
- Create Date: 2018-07-29 13:16:19
- Modify Date: 2024-01-08 12:44:06
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Zafirlukast is a potent orally active leukotriene D4 (LTD4) receptor antagonist.
| Name | zafirlukast |
|---|---|
| Synonyms |
Cyclopentyl [3-(2-methoxy-4-{[(2-methylphenyl)sulfonyl]carbamoyl}benzyl)-1-methyl-1H-indol-5-yl]carbamate
Vanticon Accoleit Cyclopentyl [3-[2-Methoxy-4-[(o-tolylsulfonyl)carbamoyl]benzyl]-1-methyl-1H-indol-5-yl]carbamate carbamic acid, [3-[[2-methoxy-4-[[[(2-methylphenyl)sulfonyl]amino]carbonyl]phenyl]methyl]-1-methyl-1H-indol-5-yl]-, cyclopentyl ester Cyclopentyl 3-[2-methoxy-4-({[(2-methylphenyl)sulfonyl]amino}carbonyl)benzyl]-1-methyl-1H-indol-5-ylcarbamate Zafirlukast Cyclopentyl (3-(2-methoxy-4-((o-tolylsulfonyl)carbamoyl)benzyl)-1-methyl-1H-indol-5-yl)carbamate Accolate cyclopentyl (1-methyl-3-{[2-(methyloxy)-4-({[(2-methylphenyl)sulfonyl]amino}carbonyl)phenyl]methyl}-1H-indol-5-yl)carbamate Carbamic acid, N-[3-[[2-methoxy-4-[[[(2-methylphenyl)sulfonyl]amino]carbonyl]phenyl]methyl]-1-methyl-1H-indol-5-yl]-, cyclopentyl ester MFCD00864775 |
| Description | Zafirlukast is a potent orally active leukotriene D4 (LTD4) receptor antagonist. |
|---|---|
| Related Catalog | |
| Target |
LTD4 |
| In Vivo | Zafirlukast is a peptidyl leukotriene antagonist and inhibitor of LTD4. After 13 weeks of exposure, the yield of lung tumors is significantly decreased by both dose levels of Zafirlukast (270 and 540 mg/kg), the high dose of Zileuton (1200 mg/kg), and the combinations containing 600 mg/kg Zileuton with either Zafirlukast or MK-866. The efficacy of the combination containing Zileuton and Zafirlukast to prevent lung tumors is not significantly different from the efficacy of either inhibitor administered alone. Although when administered alone at the dose level in their combination, neither Zileuton or MK-886 prevents lung tumors; the combination containing them does significantly prevent tumors. In contrast, the combination containing Zafirlukast and MK-886 does not reduce the yield of tumors, whereas Zafirlukast administered alone does significantly reduce the yield of tumors[2]. |
| Animal Admin | Mice[2] Female A/J mice (5-6 weeks of age) are used. When the mice are 7-8 weeks of age, they are administered the first of two i.p. injections of vinyl carbamate of 16 mg/kg each and 7 days apart. Two weeks after the second dose of vinyl carbamate, the mice receive the leukotriene inhibitors in their diet. Zafirlukast (270 or 540 mg/kg), Zileuton (600 or 1200 mg/kg), and MK-886 (30 mg/kg) is provided at the indicated mg/kg concentrations in the diet. Mice are weighed weekly through the first 6 weeks of exposure to the leukotriene inhibitors. After which, they are then weighed every 2-4 weeks until sacrificed. Mice are sacrificed by carbon dioxide asphyxiation after 13 and 43 weeks of exposure to the drugs. The lungs are harvested, fixed overnight in formalin, transferred to 70% alcohol, and evaluated for tumors before embedding in paraffin for histology[1]. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Melting Point | 139°C |
| Molecular Formula | C31H33N3O6S |
| Molecular Weight | 575.675 |
| Exact Mass | 575.208984 |
| PSA | 131.09000 |
| LogP | 6.15 |
| Index of Refraction | 1.641 |
| Storage condition | Refrigerator |
| Precursor 10 | |
|---|---|
| DownStream 0 | |
![4-[[5-[[cyclopentyloxy)carbonyl]amino]-1-methylindol-3-yl]methyl]-3-methoxybenzoic acid structure](https://image.chemsrc.com/caspic/193/107754-20-1.png)
![4-[5-nitro-1H-indol-3-ylmethyl]-3-methoxy-benzoic acid methylester structure](https://image.chemsrc.com/caspic/101/107786-36-7.png)
![4-[[5-[[(Cyclopentyloxy)carbonyl]amino]-1-Methyl-1H-indol-3-yl]Methyl]-3-Methoxy-benzoic Acid Methyl Ester structure](https://image.chemsrc.com/caspic/058/107754-19-8.png)
