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PF-9184

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Catalog No. T21738Cas No. 1221971-47-6

PF-9184 is a potent and selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 16.5 nM, and it inhibits IL-1β-induced PGE2 synthesis in vitro.

PF-9184

PF-9184

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Purity: 97.43%
Catalog No. T21738Cas No. 1221971-47-6
PF-9184 is a potent and selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 16.5 nM, and it inhibits IL-1β-induced PGE2 synthesis in vitro.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$30In StockIn Stock
5 mg$69In StockIn Stock
10 mg$105In StockIn Stock
25 mgPreferentialIn StockIn Stock
50 mgPreferentialIn 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.
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:97.43%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
PF-9184 is a potent and selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 16.5 nM, and it inhibits IL-1β-induced PGE2 synthesis in vitro.
In vitro
PF-9184 (0.015-100 μM; 24 hours) inhibits IL-1β-stimulated prostaglandin E2 (PGE2) synthesis in synovial fibroblasts derived from rheumatoid arthritis (RASF) patients with no apparent cytotoxic effects. It potently blocks mPGES-1's ability to synthesize PGE2 from PGH2 without inhibiting COX-2 and prostacyclin synthase in cells. In human whole blood and modified blood assays, PF-9184 weakly inhibits PGE2 and affects TXB2 synthesis only at 100 μM. PF-9184 poorly inhibits recombinant rat mPGES-1 (IC50=1080±398 nM)[1].
In vivo
PF-9184, whether administered orally or locally, does not affect PGE2 synthesis in recombinant rats[1].
Chemical Properties
Molecular Weight461.32
FormulaC21H14Cl2N2O4S
Cas No.1221971-47-6
SmilesOC1=C(NS(=O)(=O)c2ccccc12)C(=O)Nc1ccc(cc1)-c1ccc(Cl)c(Cl)c1
Relative Density.1.574 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: 60 mg/mL (130.06 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1677 mL10.8385 mL21.6769 mL108.3846 mL
5 mM0.4335 mL2.1677 mL4.3354 mL21.6769 mL
10 mM0.2168 mL1.0838 mL2.1677 mL10.8385 mL
20 mM0.1084 mL0.5419 mL1.0838 mL5.4192 mL
50 mM0.0434 mL0.2168 mL0.4335 mL2.1677 mL
100 mM0.0217 mL0.1084 mL0.2168 mL1.0838 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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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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