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GSK2239633A

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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

GSK2239633A

🥰Excellent
Purity: 99.78%
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 SizePriceAvailabilityQuantity
1 mg30 €In Stock
5 mg72 €In Stock
10 mg120 €In Stock
25 mg259 €In Stock
50 mg375 €In Stock
100 mg544 €In Stock
500 mgInquiryIn Stock
1 mL x 10 mM (in DMSO)89 €In Stock
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Purity:99.78%
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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 Weight549.06
FormulaC24H25ClN4O5S2
Cas No.1240516-71-5
SmilesCOc1cccc2n(Cc3cccc(CNC(=O)C(C)(C)O)c3)nc(NS(=O)(=O)c3ccc(Cl)s3)c12
Relative Density.1.45 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 250 mg/mL (455.32 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8213 mL9.1065 mL18.2129 mL91.0647 mL
5 mM0.3643 mL1.8213 mL3.6426 mL18.2129 mL
10 mM0.1821 mL0.9106 mL1.8213 mL9.1065 mL
20 mM0.0911 mL0.4553 mL0.9106 mL4.5532 mL
50 mM0.0364 mL0.1821 mL0.3643 mL1.8213 mL
100 mM0.0182 mL0.0911 mL0.1821 mL0.9106 mL

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