| 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. |
| In vitro | GSK2239633A提升了人类CD4+ CCR4+ T细胞在CCL17诱导下的F-actin含量，其pEC50值为8.79±0.22[1]。此外，GSK2239633A抑制了胸腺和活化调节化学趋化因子(TARC)诱导的人类CD4+ CCR4+ T细胞F-actin含量增加，其pA2值为7.11±0.29[3]。 |
| In vivo | GSK2239633A在预临床动物研究中展现出良好的药代动力学数据，大鼠和比格犬的生物利用度分别为85%和97%[2]。血浆中GSK2239633A（静脉注射）显示出快速的、双相分布，并且终末消除缓慢（13.5小时），表明GSK2239633A是一种低至中等清除率的化合物。GSK2239633A（口服）血药浓度迅速达到最大浓度（中位tmax：1.0-1.5小时）[3]。 |
| Target activity | [125I]-TARC-CCR4:7.96(pIC50) |
| molecular weight | 549.06 |
| Molecular formula | C24H25ClN4O5S2 |
| CAS | 1240516-71-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 250 mg/mL (455.32 mM) |
| References | 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. |