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Gemilukast

Name: Gemilukast
Brand: TargetMol
SKU: T11388
Price: 117 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11388Cas No. 1232861-58-3

Alias 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.

Gemilukast

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Purity: 99.5%

Catalog No. T11388Alias ONO-6950Cas No. 1232861-58-3

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$117	-	In Stock
5 mg	$289	-	In Stock
10 mg	$496	-	In Stock
25 mg	$962	-	In Stock
50 mg	$1,490	-	In Stock
100 mg	$2,650	-	In Stock
1 mL x 10 mM (in DMSO)	$382	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.5%

Appearance:Solid

Color:White

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COA LCMS

Product Introduction

Bioactivity

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	CysLT1:1.7 nM (Human), CysLT2:25 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

Chemical Properties

Molecular Weight	601.68
Formula	C₃₆H₃₇F₂NO₅
Cas No.	1232861-58-3
Smiles	Cc1c(CCCC(O)=O)c2c(F)ccc(C#Cc3ccc(OCCCCc4cccc(F)c4C)cc3)c2n1CCCC(O)=O
Relative Density.	1.18 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (166.2 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (6.65 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6620 mL	8.3101 mL	16.6201 mL	83.1007 mL
5 mM	0.3324 mL	1.6620 mL	3.3240 mL	16.6201 mL
10 mM	0.1662 mL	0.8310 mL	1.6620 mL	8.3101 mL
20 mM	0.0831 mL	0.4155 mL	0.8310 mL	4.1550 mL
50 mM	0.0332 mL	0.1662 mL	0.3324 mL	1.6620 mL
100 mM	0.0166 mL	0.0831 mL	0.1662 mL	0.8310 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc