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BMS582949

Name: BMS582949
Brand: TargetMol
SKU: T6789
Price: 79 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6789Cas No. 623152-17-0

Alias PS540446, BMS-582949, BMS 582949

BMS-582949 is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13 nM, inhibiting both p38 kinase activity and activation of p38.

BMS582949

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Purity: 98.11%

Catalog No. T6789Alias PS540446, BMS-582949, BMS 582949Cas No. 623152-17-0

BMS-582949 is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13 nM, inhibiting both p38 kinase activity and activation of p38.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$79	In Stock	In Stock
2 mg	$123	In Stock	In Stock
5 mg	$222	In Stock	In Stock
10 mg	$315	In Stock	In Stock
25 mg	$529	In Stock	In Stock
50 mg	$768	In Stock	In Stock
100 mg	$1,080	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$222	In Stock	In Stock

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

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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Batch Information

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Purity:98.11%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	BMS-582949 is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13 nM, inhibiting both p38 kinase activity and activation of p38.
Targets&IC50	p38 MAPK (cell-free assay):13 nM
In vitro	BMS-582949 is found to inhibit p38 activation in cells, as measured by phosphorylation of p38. BMS-582949 treatment of cells in which p38 has been activated by LPS rapidly reversed p38 activation as shown by loss of phosphorylation of p38. BMS-582949 is therefore a dual action p38 kinase inhibitor, inhibiting both p38 kinase activity and p38 activation in cells. BMS-582949 binding to p38a results in a conformational change of the activation loop which is phosphorylated by upstream kinases, therefore it inhibits phosphorylation of p38 by upstream MKK by inducing a less accessible conformation of the activation loop[2].
In vivo	The mouse clearance rate for BMS-582949 is 4.4 mL/min/kg. And at an oral dose of 10 mg/kg, the mouse AUC0-8 h for BMS-582949 is 75.5 μM?h. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively[1].
Kinase Assay	Autophosphorylation activity is measured by adding of 32P-γ ATP. Endonuclease activity is measured by the adding of radiolabeled HAC1 508-nt RNA substrate synthesized in vitro using α32P-UTP. Mix STF083010 with recombinant hIRE1 protein, radiolabeled HAC1 508 nt RNA, and appropriate buffers to incubate. Kinase activity is quantitated by polyacrylamide gel electrophoresis. RNAsecleavage products are quantitated by 32P-γATP or 32P-UTP autoradiography.
Synonyms	PS540446, BMS-582949, BMS 582949

Chemical Properties

Molecular Weight	406.48
Formula	C₂₂H₂₆N₆O₂
Cas No.	623152-17-0
Smiles	N(C=1C=2N(C=C(C(NCCC)=O)C2C)N=CN1)C3=CC(C(NC4CC4)=O)=CC=C3C
Relative Density.	no data available

Storage & Solubility Information

Storage

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

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 75 mg/mL (184.51 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4601 mL	12.3007 mL	24.6015 mL	123.0073 mL
5 mM	0.4920 mL	2.4601 mL	4.9203 mL	24.6015 mL
10 mM	0.2460 mL	1.2301 mL	2.4601 mL	12.3007 mL
20 mM	0.1230 mL	0.6150 mL	1.2301 mL	6.1504 mL
50 mM	0.0492 mL	0.2460 mL	0.4920 mL	2.4601 mL
100 mM	0.0246 mL	0.1230 mL	0.2460 mL	1.2301 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