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GSK2239633A
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.
Catalog No. T11481Cas No. 1240516-71-5
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Purity:99.78%
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GSK2239633A
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.
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. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 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 | Inquiry | In Stock | |
| 1 mL x 10 mM (in DMSO) | $94 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
| 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 & Solubility Information
| 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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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 . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (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.
(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 main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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