CAS NO: | 1232861-58-3 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors(CysLT1and CysLT2)antagonist, withIC50sof 1.7, 25 nM for humanCysLT1andCysLT2, respectively. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1and CysLT2, respectively[1]. Both Gemilukast (ONO-6950) and montelukast inhibit human CysLT1receptor-mediated calcium response with IC50values of 1.7 and 0.46 nM, respectively[2]. | ||||||||||||||||
体内研究 (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]. | ||||||||||||||||
分子量 | 601.68 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C36H37F2NO5 | ||||||||||||||||
CAS 号 | 1232861-58-3 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(415.50 mM;Need ultrasonic) 配制储备液
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