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Atuliflapon

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Catalog No. T9023Cas No. 2041075-86-7
Alias AZD5718

Atuliflapon (AZD5718) is a novel 5-Lipoxygenase Activating Protein(FLAP) inhibitor for Treatment of Coronary Artery Disease.

Atuliflapon

Atuliflapon

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Purity: 99.28%
Catalog No. T9023Alias AZD5718Cas No. 2041075-86-7
Atuliflapon (AZD5718) is a novel 5-Lipoxygenase Activating Protein(FLAP) inhibitor for Treatment of Coronary Artery Disease.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$44In StockIn Stock
5 mg$98In StockIn Stock
10 mg$158In StockIn Stock
25 mg$268In StockIn Stock
50 mg$371In StockIn Stock
100 mg$476In StockIn Stock
200 mg$666-In Stock
1 mL x 10 mM (in DMSO)$107In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.28%
Appearance:Solid
Color:White
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Product Introduction

Atuliflapon AI Summary
Atuliflapon exhibits promising bioactivities with potential therapeutic applications, particularly in anti-inflammatory treatments. It demonstrates high inhibition potential against FLAP activity in human systems, with IC50 values of 6.3 nM and fIC50 values of 2.0 nM. In rat systems, it shows moderate inhibition of Mrp2 and BSEP with IC50 values of 74,000.0 nM. The compound has good oral bioavailability and clearance rates in both rats and Beagle dogs, indicating effective systemic uptake and metabolism. It also displays low cytotoxicity in human THP1 and HepG2 cells, with IC50 values exceeding 250,000.0 nM. Selectively inhibiting FLAP activity over COX1 and COX2 in human whole blood, it shows effective ex vivo inhibition in Beagle dogs through reductions in LTB4 and LTE4 levels. Pharmacokinetic properties are favorable, with a half-life of 12.0 hours in humans and 2.1 hours in Beagle dogs post intravenous administration. Additionally, it significantly suppresses calcium ionophore-stimulated LTB4 production at concentrations as low as 15.0 nM in human systems. These findings underscore Atuliflapon's strong anti-inflammatory properties, selective FLAP inhibition, and excellent pharmacokinetic profile, making it a viable candidate for further therapeutic development..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Atuliflapon (AZD5718) is a novel 5-Lipoxygenase Activating Protein(FLAP) inhibitor for Treatment of Coronary Artery Disease.
Targets&IC50
FLAP:2 nM (IC50)
SynonymsAZD5718
Chemical Properties
Molecular Weight446.5
FormulaC24H26N6O3
Cas No.2041075-86-7
SmilesCc1cc(n[nH]1)-c1ccc(cc1)C(=O)[C@@H]1CCCC[C@H]1C(=O)Nc1cnn2CCNC(=O)c12
Relative Density.1.48 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 25 mg/mL (55.99 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.48 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 mM2.2396 mL11.1982 mL22.3964 mL111.9821 mL
5 mM0.4479 mL2.2396 mL4.4793 mL22.3964 mL
10 mM0.2240 mL1.1198 mL2.2396 mL11.1982 mL
20 mM0.1120 mL0.5599 mL1.1198 mL5.5991 mL
50 mM0.0448 mL0.2240 mL0.4479 mL2.2396 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:
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2 Enter the in vivo formulation:
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%
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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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