| Name | Gemilukast |
| Description | Gemilukast (ONO-6950) is an orally active and potent dual inhibitor of cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2), inhibits LTC 4-induced bronchoconstriction, and is inhibitory to human CysLT1 and CysLT2, and may be used in the treatment of asthma. |
| In vitro | Gemilukast is a potent dual antagonist for cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2), and it is orally active. It exhibits IC50 values of 1.7 nM and 25 nM for human CysLT1 and CysLT2, respectively[2]. In comparison, both Gemilukast (ONO-6950) and montelukast inhibit the human CysLT1 receptor-mediated calcium response, with IC50 values of 1.7 nM and 0.46 nM, respectively[1]. |
| In vivo | Orally administered Gemilukast, at doses ranging from 0.03 to 10 mg/kg, demonstrates a dose-dependent attenuation of LTC4-induced bronchoconstriction, reaching almost complete inhibition at 3 mg/kg. Notably, Gemilukast's inhibitory effect on LTC4-induced bronchoconstriction is significantly stronger than that observed with montelukast at doses equal to or greater than 1 mg/kg.Furthermore, Gemilukast (at doses from 0.03 to 1 mg/kg, p.o.) dose-dependently attenuates LTD4-induced airway vascular hyperpermeability, achieving complete inhibition at 0.3 mg/kg. In the context of OVA-induced bronchoconstriction, Gemilukast at doses ranging from 0.1 to 3 mg/kg, p.o., exhibits a dose-dependent inhibitory effect. Particularly, the inhibitory effect of Gemilukast at 3 mg/kg surpasses that of montelukast alone and is comparable to the combination therapy involving montelukast and BayCysLT2RA[2]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 100 mg/mL (166.2 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (6.65 mM), Sonication is recommended.
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| Keywords | ONO6950 | ONO 6950 | Gemilukast | CysLTR | CysLT2 | CysLT1 |
| Inhibitors Related | Moxilubant HCl | Montelukast sodium | LTB4-IN-1 | L 674573 | Olsalazine disodium | Pirodomast | Pranlukast | Desloratadine | CGP 35949 | ABT-080 | Darbufelone mesylate | Ticolubant |
| Related Compound Libraries | Bioactive Compound Library | ReFRAME Related Library | Drug Repurposing Compound Library | Inhibitor Library | Orally Active Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | GPCR Compound Library |
United States
