1232861-58-3
1232861-58-3 structure
- Name: Gemilukast
- Chemical Name: gemilukast
- CAS Number: 1232861-58-3
- Molecular Formula: C36H37F2NO5
- Molecular Weight: 601.680
- Catalog: Signaling Pathways GPCR/G Protein Leukotriene Receptor
- Create Date: 2018-06-13 03:40:23
- Modify Date: 2025-08-21 05:55:42
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Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively.
| Name | gemilukast |
|---|---|
| Synonyms |
gemilukast
4,4'-[4-Fluoro-7-({4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl}ethynyl)-2-methyl-1H-indole-1,3-diyl]dibutanoic acid 1H-Indole-1,3-dibutanoic acid, 4-fluoro-7-[2-[4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methyl- |
| Description | Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively. |
|---|---|
| Related Catalog | |
| Target |
CysLT1:1.7 nM (IC50, in human) CysLT2:25 nM (IC50, in human) |
| In Vitro | Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively[1]. Both Gemilukast (ONO-6950) and montelukast inhibit human CysLT1 receptor-mediated calcium response with IC50 values of 1.7 and 0.46 nM, respectively[2]. |
| In Vivo | Gemilukast at 0.03 to 10 mg/kg, p.o. dose-dependently attenuates LTC4-induced bronchoconstriction with almost complete inhibition at 3 mg/kg. The inhibitory effect of Gemilukast on LTC4-induced bronchoconstriction is significantly stronger than that of montelukast at the dose of 1 mg/kg or more. Gemilukast (0.03 to 1 mg/kg, p.o.) dose-dependently attenuates LTD4-induced airway vascular hyperpermeability with complete inhibition at 0.3 mg/kg. Gemilukast at 0.1 to 3 mg/kg, p.o. dose-dependently inhibits OVA-induced bronchoconstriction. The inhibitory effect of Gemilukast at 3 mg/kg is significantly greater than that of montelukast alone and comparable to that of combination therapy with montelukast and BayCysLT2RA[2]. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 806.6±65.0 °C at 760 mmHg |
| Molecular Formula | C36H37F2NO5 |
| Molecular Weight | 601.680 |
| Flash Point | 441.6±34.3 °C |
| Exact Mass | 601.263977 |
| LogP | 9.21 |
| Vapour Pressure | 0.0±3.0 mmHg at 25°C |
| Index of Refraction | 1.570 |