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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 | Quantity |
---|---|---|---|
1 mg | 30 € | In Stock | |
5 mg | 72 € | In Stock | |
10 mg | 120 € | In Stock | |
25 mg | 259 € | In Stock | |
50 mg | 375 € | In Stock | |
100 mg | 544 € | In Stock | |
500 mg | Inquiry | In Stock | |
1 mL x 10 mM (in DMSO) | 89 € | In Stock |
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 |
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) |
Storage | Powder: -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
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