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GSK2239633A

Catalog No. T11481   CAS 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.

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GSK2239633A Chemical Structure
GSK2239633A, CAS 1240516-71-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 54.00
5 mg In stock $ 128.00
10 mg In stock $ 213.00
25 mg In stock $ 455.00
50 mg In stock $ 672.00
100 mg In stock $ 956.00
500 mg In stock $ 1,920.00
1 mL * 10 mM (in DMSO) In stock $ 157.00
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Purity: 99.78%
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Biological Description
Chemical Properties
Storage & Solubility Information
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].
Molecular Weight 549.06
Formula C24H25ClN4O5S2
CAS No. 1240516-71-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 250 mg/mL (455.32 mM)

TargetMolReferences and Literature

1. Slack RJ, et al. Antagonism of human CC-chemokine receptor 4 can be achieved through three distinct binding sites on the receptor. Pharmacol Res Perspect. 2013 Dec;1(2):e00019. 2. Miah AH, et al. Identification of pyrazolopyrimidine arylsulfonamides as CC-chemokine receptor 4 (CCR4) antagonists. Bioorg Med Chem. 2017 Oct 15;25(20):5327-5340. 3. Cahn A, et al. Safety, tolerability, pharmacokinetics and pharmacodynamics of GSK2239633, a CC-chemokine receptor 4 antagonist, in healthy male subjects: results from an open-label and from a randomised study. BMC Pharmacol Toxicol. 2013 Feb 28;14:14.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library ReFRAME Related Library Inhibitor Library Bioactive Compounds Library Max Immuno-Oncology Compound Library

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Keywords

GSK2239633A 1240516-71-5 Immunology/Inflammation Microbiology/Virology CCR GSK-2239633A inhibit Inhibitor CC chemokine receptor inhibitor

 

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