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1mg |
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5mg |
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10mg |
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Other Sizes |
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Purity: ≥98%
Gemilukast (formerly also known as ONO-6950) is a novel, potent and orally bioavailable dual CysLT1 and CysLT2 (cysteinyl leukotriene 1 and 2) antagonist with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively.. Gemilukast exhibited potent in vivo efficacy at an oral dose of 0.1 mg/kg given 24 h before LTD4 challenge in a CysLT1-dependent guinea pig asthmatic model. In addition, gemilukast dose-dependently reduced LTC4-induced bronchoconstriction in both CysLT1- and CysLT2-dependent guinea pig asthmatic models, and it reduced antigen-induced constriction of isolated human bronchi. Gemilukast is currently being evaluated in phase II trials for the treatment of asthma.
ln Vitro |
Gemilukast is an orally active antagonist of the human biscysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2), with IC50 values of 1.7 and 25 nM, respectively [1]. Both gemilukast (ONO-6950) and montelukast, with IC50 values of 1.7 and 0.46 nM, respectively, block the calcium response mediated by the human CysLT1 receptor [2].
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ln Vivo |
Oral dosing of 0.03 to 10 mg/kg gimilukast dosage-dependently reduced LTC4-induced bronchoconstriction, with practically full inhibition at a dose of 3 mg/kg. At dosages of 1 mg/kg or above, the inhibitory impact of gemilukast on LTC4-induced bronchoconstriction was substantially stronger than that of montelukast. Gemilukast (0.03 to 1 mg/kg, orally) dose-dependently decreased LTD4-induced airway vascular hyperpermeability and was entirely suppressed at 0.3 mg/kg. Oral treatment of 0.1 to 3 mg/kg of gemimirukast dose-dependently reduced OVA-induced bronchoconstriction. The inhibitory impact of 3 mg/kg gimelukast was substantially greater than that of montelukast alone and was comparable to the combined therapy of montelukast and BayCysLT2RA [2].
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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. |
CAS # |
1232861-58-3
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Related CAS # |
1232861-58-3 (free acid);1232861-64-1 (disodium);1232873-69-6 (8 hydrate and disodium);
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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
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InChi Key |
SILHYVDKGHXGBL-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C36H37F2NO5/c1-24-27(9-5-11-31(24)37)8-3-4-23-44-29-19-15-26(16-20-29)14-17-28-18-21-32(38)35-30(10-6-12-33(40)41)25(2)39(36(28)35)22-7-13-34(42)43/h5,9,11,15-16,18-21H,3-4,6-8,10,12-13,22-23H2,1-2H3,(H,40,41)(H,42,43)
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Chemical Name |
4,4'-(4-fluoro-7-((4-(4-(3-fluoro-2-methylphenyl)butoxy)phenyl)ethynyl)-2-methyl-1H-indole-1,3-diyl)dibutyric acid
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Synonyms |
ONO-6950; ONO 6950; ONO6950
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~250 mg/mL (~415.50 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.46 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.