Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT 1 and CysLT 2 ) antagonist, with IC 50 s of 1.7, 25 nM for human CysLT 1 and CysLT 2 , respectively. In Vitro Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT 1 and CysLT 2 ) antagonist, with IC 50 s of 1.7, 25 nM for human CysLT 1 and CysLT 2 , respectively. Both Gemilukast (ONO-6950) and montelukast inhibit human CysLT 1 receptor-mediated calcium response with IC 50 values of 1.7 and 0.46 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:CysLT 1 1.7 nM (IC 50 , in human) CysLT 2 25 nM (IC 50 , in human)
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
Gemilukast
CAS number：1232861-58-3(DMSO) molecular formula：C36H37F2NO5
overview
compound introduction
Specs
| Chinese alias | 吉米司特 | ||
| English alias | - | ||
| CAS number | 1232861-58-3(DMSO) | molecular formula | C36H37F2NO5 |
| molecular weight | 601.68 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
