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GSK2239633A

Name: GSK2239633A
Brand: TargetMol
SKU: T11481
Price: 573 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11481Cas No. 1240516-71-5

GSK2239633A is an allosteric antagonist of CC-chemokine receptor 4 (CCR4) with a pIC50 of 7.96 for the binding of [125I]-TARC to human CCR4.

GSK2239633A

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Purity: 99.82%

Catalog No. T11481Cas No. 1240516-71-5

GSK2239633A is an allosteric antagonist of CC-chemokine receptor 4 (CCR4) with a pIC50 of 7.96 for the binding of [125I]-TARC to human CCR4.

Pack Size	Price	Availability
1 mg	$32	In Stock
5 mg	$76	In Stock
10 mg	$127	In Stock
25 mg	$273	In Stock
50 mg	$395	In Stock
100 mg	$573	In Stock
500 mg	Preferential	In Stock
1 mL x 10 mM (in DMSO)	$94	In Stock

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Purity:99.82%

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	GSK2239633A is an allosteric antagonist of CC-chemokine receptor 4 (CCR4) with a pIC50 of 7.96 for the binding of [125I]-TARC to human CCR4.
Targets&IC50	[125I]-TARC-CCR4:7.96(pIC50)
In vitro	GSK2239633A increases the CCL17-induced F-actin content of human CD4+ CCR4+ T cells with a pEC50 value of 8.79±0.22[1]. GSK2239633A inhibits thymus- and activation-regulated chemokine-induced (TARC)-induced increases in the F-actin content of isolated human CD4+ CCR4+ T-cells with a pA2 of 7.11±0.29[3].
In vivo	GSK2239633A demonstrates good pharmacokinetic data in preclinical animal studies with bioavailability in rats and beagle dogs of 85% and 97% respectively[2]. Plasma GSK2239633A (i.v.) displays rapid, bi-phasic distribution and slow terminal elimination (13.5 h), suggesting that GSK2239633A is a low to moderate clearance drug. Blood levels of GSK2239633A(oral) reach Cmax rapidly (median tmax: 1.0-1.5 hours)[3].

Chemical Properties

Molecular Weight	549.06
Formula	C₂₄H₂₅ClN₄O₅S₂
Cas No.	1240516-71-5
Smiles	COc1cccc2n(Cc3cccc(CNC(=O)C(C)(C)O)c3)nc(NS(=O)(=O)c3ccc(Cl)s3)c12
Relative Density.	1.45 g/cm3 (Predicted)
Color	White
Appearance	Solid

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (455.32 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8213 mL	9.1065 mL	18.2129 mL	91.0647 mL
5 mM	0.3643 mL	1.8213 mL	3.6426 mL	18.2129 mL
10 mM	0.1821 mL	0.9106 mL	1.8213 mL	9.1065 mL
20 mM	0.0911 mL	0.4553 mL	0.9106 mL	4.5532 mL
50 mM	0.0364 mL	0.1821 mL	0.3643 mL	1.8213 mL
100 mM	0.0182 mL	0.0911 mL	0.1821 mL	0.9106 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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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