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Gemilukast(ONO-6950)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Gemilukast(ONO-6950)图片
CAS NO:1232861-58-3
规格:98%
分子量:601.68
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
Gemilukast是具有口服活性的、有效的半胱氨酰白三烯1和2受体(CysLT1和CysLT2)的双抑制剂,其对人CysLT1和CysLT2的IC50值分别为1.7nM和25nM。
CAS:1232861-58-3
分子式:C36H37F2NO5
分子量:601.68
纯度:98%
存储:Store at -20°C

Background:

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.


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].


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].


[1]. Itadani S, et al. Discovery of Gemilukast (ONO-6950), a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma. J Med Chem. 2015 Aug 13;58(15):6093-113. [2]. Yonetomi Y, et al. Effects of ONO-6950, a novel dual cysteinyl leukotriene 1 and 2 receptors antagonist, in a guinea pig model of asthma. Eur J Pharmacol. 2015 Oct 15;765:242-8.