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Nemiralisib

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Catalog No. T15431Cas No. 1254036-71-9
Alias GSK2269557

Nemiralisib(GSK-2269557 free base) is an orally available, potent and specific PI3Kδ inhibitor with a pKi of 9.9.Nemiralisib is used for the treatment of respiratory diseases including chronic obstructive pulmonary disease.

Nemiralisib

Nemiralisib

😃Good
Purity: 99.91%
Catalog No. T15431Alias GSK2269557Cas No. 1254036-71-9
Nemiralisib(GSK-2269557 free base) is an orally available, potent and specific PI3Kδ inhibitor with a pKi of 9.9.Nemiralisib is used for the treatment of respiratory diseases including chronic obstructive pulmonary disease.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$40In StockIn Stock
2 mg$56In StockIn Stock
5 mg$91In StockIn Stock
10 mg$147-In Stock
25 mg$297-In Stock
50 mg$476-In Stock
1 mL x 10 mM (in DMSO)$100In StockIn 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.
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Purity:99.91%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
Nemiralisib(GSK-2269557 free base) is an orally available, potent and specific PI3Kδ inhibitor with a pKi of 9.9.Nemiralisib is used for the treatment of respiratory diseases including chronic obstructive pulmonary disease.
Targets&IC50
PI3Kδ:9.9 (pki), PI3Kβ:5.8 (pic50), PI3Kα:5.3 (pic50), PI3Kγ:5.2 (pic50)
In vitro
Nemiralisib inhibits IFNγ in the peripheral blood mononuclear (PBMC) (pIC50: 9.7). Nemiralisib is highly selective for PI3Kδ. It has >1000-fold selectivity over the closely related isoforms PI3Kα (pIC50: 5.3), PI3Kβ (pIC50: 5.8), and PI3Kγ (pIC50: 5.2).[1]
In vivo
Nemiralisib is active in a disease-relevant brown Norway rat acute OVA model of Type 2 helper T-cells (Th2)-driven lung inflammation. Pharmacokinetic data from Sprague Dawley male rats are obtained to assess the suitability of the series for inhaled delivery clearance data in rat microsomes and subsequently in vivo. Compounds (e.g., Nemiralisib) are administered by the oral or intravenous routes, at a dose level of 3 and 1mg/kg respectively (n=2 rats/route).[1]
SynonymsGSK2269557
Chemical Properties
Molecular Weight440.54
FormulaC26H28N6O
Cas No.1254036-71-9
SmilesCC(C)N1CCN(Cc2cnc(o2)-c2cc(cc3[nH]ncc23)-c2cccc3[nH]ccc23)CC1
Relative Density.1.281 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 29 mg/mL (65.83 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.54 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
1mg5mg10mg50mg
1 mM2.2699 mL11.3497 mL22.6994 mL113.4971 mL
5 mM0.4540 mL2.2699 mL4.5399 mL22.6994 mL
10 mM0.2270 mL1.1350 mL2.2699 mL11.3497 mL
20 mM0.1135 mL0.5675 mL1.1350 mL5.6749 mL
50 mM0.0454 mL0.2270 mL0.4540 mL2.2699 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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

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