Elacridar (GG918) is a potent inhibitor of P-glycoprotein and BCRP.

方法： MCF-7、Caki-1 和 786-O 细胞系用Elacridar (GG918)（5μM，24小时），制备细胞裂解物并装入每个孔中，通过免疫印迹确定蛋白质表达，检测 β-肌动蛋白的表达以标准化总蛋白质负载。
结果：Elacridar (GG918)影响MCF-7和786-O细胞系中的P-糖蛋白和ABCG2蛋白表达水平；影响Tc-MIBI在MCF-7和786-O细胞中的细胞内积累。[2]

方法：Elacridar (GG918)以三种不同的给药方式（2.5mg/kg，静脉注射；100mg/kg，腹腔注射；100mg/kg，口服）给FVB 野生型小鼠，研究Elacridar (GG918) 在血浆和大脑中的药代动力学参数。
结果：Elacridar (GG918)在三种给药方式中血浆和大脑中的药代动力学参数不同：静脉注射给药血浆中半衰期为 4.4 小时，脑中为 1.5 小时，Kp值为0.82；腹腔注射血浆中半衰期为 4.3 小时，脑中为 9.2小时，Kp值为0.48；腹腔注射血浆中半衰期为 20 小时，脑中为 16小时，Kp值为4.31。[1]

Photoaffinity radiolabeling of P-gp: 10 μL of unlabeled cell membrane suspension (at 0.4 mg of protein/mL) are aliquoted into each well in 96-well plates. 5 μL of GF120918 are then added to each well. The plate is incubated 25 min at 25℃ in the dark. 5 μL of tritiated azidopine (1.8 TBq/mmol) (0.6 μM in HCI 0.2 mM) are added to each well. After 25 min of incubation at 25℃ in the dark, samples are simultaneously irradiated for 2 min at 254 nm at 0℃ with a thin layer chromatography-designed UV lamp directly in contact with the plate. Samples are solubilized in sodium dodecyl sulfate-polyacrylamide gel electrophoresis sample buffer but not heated. After separation on a 7.5% polyacrylamide gel, the gel is treated for fluorography with Amplify and exposed during 3 days onto a photosensitive film. The fluorography is analysed using a Camag thin layer chromatography Scanner II densitometer.

3.0×103 cells per well are seeded in a 96-well plate. After 24 h incubation, an optimum concentration gradient of elacridar is added to each well. After culturing for 48 h, cell viability is assessed using the proliferation reagent, MTT. Control cells are treated with the vehicle only, 0.1% DMSO. After this ?nal incubation, the medium is aspirated and precipitated formazan crystals are dissolved in DMSO (100 μL/well). The absorbance of each well is measured at 540 nm, and a reference wavelength of 650 nm is read with a multiskan JX microplate reader. Cell viability is calculated as percentage of the control value. (Only for Reference)