[CAS NO. 1232861-58-3] Gemilukast
PRODUCTS SPECIFICATIONS [1232861-58-3]
DESCRIPTION [1232861-58-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 601.68 |
| Molecular Formula | C36H37F2NO5 |
| SMILES | O=C(O)CCCN1C(C)=C(CCCC(O)=O)C2=C1C(C#CC3=CC=C(OCCCCC4=CC=CC(F)=C4C)C=C3)=CC=C2F |
Summary
IC50 & Target
|
CysLT 1 1.7 nM (IC 50 , in human) |
CysLT 2 25 nM (IC 50 , in human) |
In Vitro
Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT 1 and CysLT 2 ) antagonist, with IC 50 s of 1.7, 25 nM for human CysLT 1 and CysLT 2 , respectively [1] . Both Gemilukast (ONO-6950) and montelukast inhibit human CysLT 1 receptor-mediated calcium response with IC 50 values of 1.7 and 0.46 nM, respectively [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 415.50 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6620 mL | 8.3101 mL | 16.6201 mL |
| 5 mM | 0.3324 mL | 1.6620 mL | 3.3240 mL |
| 10 mM | 0.1662 mL | 0.8310 mL | 1.6620 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.46 mM); Clear solution
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.