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Gemilukast

Chemical Structure : Gemilukast

CAS No.: 1232861-58-3

Gemilukast (ONO-6950;ONO6950)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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; 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); 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.

Asthma

Phase 2 Discontinued

Physicochemical Properties

M.Wt 601.69
Formula C36H37F2NO5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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

References

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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