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Pamapimod

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Catalog No. T6927Cas No. 449811-01-2
Alias Ro4402257, R1503

Pamapimod (R1503) (R-1503, Ro4402257) is a novel, selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38 gamma isoforms.

Pamapimod

Pamapimod

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Purity: 99.99%
Catalog No. T6927Alias Ro4402257, R1503Cas No. 449811-01-2
Pamapimod (R1503) (R-1503, Ro4402257) is a novel, selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38 gamma isoforms.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$51In StockIn Stock
5 mg$122In StockIn Stock
10 mg$197In StockIn Stock
25 mg$396In StockIn Stock
50 mg$635In StockIn Stock
100 mg$859-In Stock
1 mL x 10 mM (in DMSO)$133In 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:99.99%
Color:White
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Product Introduction

Bioactivity
Description
Pamapimod (R1503) (R-1503, Ro4402257) is a novel, selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38 gamma isoforms.
Targets&IC50
p38β:0.48±0.04 μM, p38α:0.014 ±0.002μM
In vitro
Pamapimod inhibited p38, but inhibition of JNK was not detected. Pamapimod also inhibited lipopolysaccharide (LPS)-stimulated tumor necrosis factor (TNF) α production by monocytes, interleukin (IL)-1β production in human whole blood, and spontaneous TNFα production by synovial explants from RA patients[1].
In vivo
In murine collagen-induced arthritis, pamapimod reduced Clinicalal signs of inflammation and bone loss at 50 mg/kg or greater. In a rat model of hyperalgesia, pamapimod increased tolerance to pressure in a dose-dependent manner, suggesting an important role of p38 in pain associated with inflammation. Pamapimod suppresses spontaneous production of TNFα by synovial explants from RA patients. LPS- and TNFα-stimulated production of TNFα and IL-6 in rodents also was inhibited by pamapimod[1].
SynonymsRo4402257, R1503
Chemical Properties
Molecular Weight406.38
FormulaC19H20F2N4O4
Cas No.449811-01-2
SmilesCn1c2nc(NC(CCO)CCO)ncc2cc(Oc2ccc(F)cc2F)c1=O
Relative Density.no data available
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
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 27 mg/mL (66.44 mM), Sonication is recommended.
DMSO: 45 mg/mL (110.73 mM), Sonication is recommended.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.4608 mL12.3038 mL24.6075 mL123.0376 mL
5 mM0.4922 mL2.4608 mL4.9215 mL24.6075 mL
10 mM0.2461 mL1.2304 mL2.4608 mL12.3038 mL
20 mM0.1230 mL0.6152 mL1.2304 mL6.1519 mL
50 mM0.0492 mL0.2461 mL0.4922 mL2.4608 mL
DMSO
1mg5mg10mg50mg
100 mM0.0246 mL0.1230 mL0.2461 mL1.2304 mL

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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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