DC Chemicals Limited
China
Product Name: Gemilukast (ONO-6950)
Price: $1500.0/100mg $3000.0/250mg $6000.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

1232861-58-3

1232861-58-3 structure

1232861-58-3 structure

Name: Gemilukast
Chemical Name: gemilukast
CAS Number: 1232861-58-3
Molecular Formula: C₃₆H₃₇F₂NO₅
Molecular Weight: 601.680
Catalog: Signaling Pathways GPCR/G Protein Leukotriene Receptor
Create Date: 2018-06-13 03:40:23
Modify Date: 2024-01-04 08:16:32
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.

Name	gemilukast
Synonyms	gemilukast 4,4'-[4-Fluoro-7-({4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl}ethynyl)-2-methyl-1H-indole-1,3-diyl]dibutanoic acid 1H-Indole-1,3-dibutanoic acid, 4-fluoro-7-[2-[4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl]ethynyl]-2-methyl-

Description	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.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Leukotriene Receptor Research Areas >> Inflammation/Immunology
Target	CysLT1:1.7 nM (IC50, in human) CysLT2:25 nM (IC50, in human)
In Vitro	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].
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].
References	[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.

Density	1.2±0.1 g/cm3
Boiling Point	806.6±65.0 °C at 760 mmHg
Molecular Formula	C₃₆H₃₇F₂NO₅
Molecular Weight	601.680
Flash Point	441.6±34.3 °C
Exact Mass	601.263977
LogP	9.21
Vapour Pressure	0.0±3.0 mmHg at 25°C
Index of Refraction	1.570