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Gemilukast

Catalog No. T11388 CAS 1232861-58-3

Synonyms: ONO-6950

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.

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Gemilukast, CAS 1232861-58-3

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1 mg	In stock	$ 189.00

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Purity: 99.5%

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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.
Targets&IC50	CysLT2:25 nM (Human), CysLT1:1.7 nM (Human)
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].

Synonyms	ONO-6950
Molecular Weight	601.68
Formula	C36H37F2NO5
CAS No.	1232861-58-3

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (166.20 mM), Sonification is recommended.

References and Literature

1. 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. 2. 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.

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Keywords

Gemilukast 1232861-58-3 Others ONO 6950 ONO-6950 ONO6950 inhibitor inhibit

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