GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [¹²⁵I]-TARC to humanCCR4with apIC₅₀of 7.96 ± 0.11.

The GSK2239633A is an allosteric antagonist of human CCR4. GSK2239633A inhibits the binding of [¹²⁵I]-TARC to human CCR4 with a pIC₅₀of 7.96±0.11 and also inhibits thymus- and activation-regulated chemokine-induced (TARC)-induced increases in the F-actin content of isolated human CD4⁺CCR4⁺T-cells with a pA₂of 7.11±0.29^[1]. The effect of GSK2239633A (Compound 3) on CCL17-induced increases in the F-actin content of human CD4⁺CCR4⁺T cells is measured. The pEC₅₀value is 8.79±0.22^[2].

Following intravenous dosing, plasma GSK2239633A displays rapid, bi-phasic distribution and slow terminal elimination (t_1/2: 13.5 hours), suggesting that GSK2239633A is a low to moderate clearance drug. Following oral dosing, blood levels of GSK2239633A reach C_maxrapidly (median t_max: 1.0-1.5 hours). Estimated GSK2239633A bioavailability is low with a maximum value determined of only 16%^[1]. GSK2239633A (Compound 9) demonstrates good pharmacokinetic data in preclinical animal studies (bioavailability in rats and beagle dogs 85% and 97% respectively)^[3].

549.06

Solid

C₂₄H₂₅ClN₄O₅S₂

1240516-71-5

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 250 mg/mL(455.32 mM)

*"≥" means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.08 mg/mL (3.79 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.79 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.08 mg/mL (3.79 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.79 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。