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首页-小分子抑制剂&激动剂-GPCR-Leukotriene Receptor-Gemilukast
Gemilukast

Chemical Structure : Gemilukast

CAS No.: 1232861-58-3

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Gemilukast (ONO-6950, ONO6950)

货号: PC-35978Not For Human Use, Lab Use Only.

Gemilukast (ONO-6950, ONO6950) is a potent, orally active, dual CysLT1 and CysLT2 antagonist with IC50 of 1.7 and 25 nM against human CysLT1 and human CysLT2, respectively.

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5 mg ￥2880 In stock
10 mg ￥4580 In stock
25 mg ￥7980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Gemilukast (ONO-6950, ONO6950) is a potent, orally active, dual CysLT1 and CysLT2 antagonist with IC50 of 1.7 and 25 nM against human CysLT1 and human CysLT2, respectively.
Gemilukast (ONO-6950) antagonized intracellular calcium signaling via human and guinea pig CysLT1 and CysLT2 receptors with IC50 values of 1.7 and 25 nM, respectively (human receptors) and 6.3 and 8.2 nM, respectively (guinea pig receptors).
Gemilukast (ONO-6950) attenuated CysLT1-mediated bronchoconstriction and airway vascular hyperpermeability induced by LTD4 in normal guinea pigs (1 or 0.3 mg/kg, p.o.), strongly inhibited this asthmatic response to the level attained by combination therapy with montelukast and BayCysLT2RA.

物理化学性质&存储条件

分子量 601.69
分子式 C36H37F2NO5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4,4'-(4-fluoro-7-((4-(4-(3-fluoro-2-methylphenyl)butoxy)phenyl)ethynyl)-2-methyl-1H-indole-1,3-diyl)dibutyric acid

参考文献

1. Itadani S, et al. J Med Chem. 2015 Aug 13;58(15):6093-113.

2. Yonetomi Y, et al. Eur J Pharmacol. 2015 Oct 15;765:242-8.

3. Gauvreau GM, et al. Allergy. 2016 Dec;71(12):1721-1727.

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