store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Elacridar (GG918) 是一种有效的 P-糖蛋白和BCRP 的抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 192 | 现货 | ||
5 mg | ¥ 389 | 现货 | ||
10 mg | ¥ 626 | 现货 | ||
25 mg | ¥ 1,130 | 现货 | ||
50 mg | ¥ 1,880 | 现货 | ||
100 mg | ¥ 3,310 | 现货 | ||
200 mg | ¥ 4,820 | 现货 | ||
500 mg | ¥ 7,580 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 529 | 现货 |
产品描述 | Elacridar (GG918) (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor. |
体外活性 | 在弗兰德白血病病毒染色的B模型小鼠中,Elacridar(2.5 mg/kg,i.v.100 mg/kg,i.p.;100 mg/kg,p.o.)在大脑-血浆中的分配系数(Kp,大脑)分别为0.82, 0.43和 4.31. 在野生型小鼠中, Elacridar(100 mg/kg,i.p.)和克唑替尼口服联用可使血浆和脑组织中克唑替尼的浓度增加,并增加克唑替尼b的大脑-血浆比值,与Abcb1a/1b; Abcg2-/-小鼠体内水平一致.在Mrp4(-/-) 模型小鼠中,Elacridar对P糖蛋白介导的托泊替康转运具有明显抑制作用,但几乎不影响Bcrp1介导的转运. |
体内活性 | 在Caki-1和 ACHN细胞中,Elacridar(2.5 μM)对细胞生长有显著抑制效果。Elacridar可抑制P-gp的活性。Elacridar抑制[3H]azidopine对P糖蛋白的标记(IC50:0.16 μM)。Elacridar与舒尼替尼联用可使ABC亚家族B分子2在786-O细胞中的表达显著降低。 |
激酶实验 | 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. |
细胞实验 | 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) |
别名 | GW0918, 依克立达, GW120918, GF120918, GG918 |
分子量 | 563.64 |
分子式 | C34H33N3O5 |
CAS No. | 143664-11-3 |
store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 41 mg/mL (72.74 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7742 mL | 8.8709 mL | 17.7418 mL | 44.3546 mL |
5 mM | 0.3548 mL | 1.7742 mL | 3.5484 mL | 8.8709 mL | |
10 mM | 0.1774 mL | 0.8871 mL | 1.7742 mL | 4.4355 mL | |
20 mM | 0.0887 mL | 0.4435 mL | 0.8871 mL | 2.2177 mL | |
50 mM | 0.0355 mL | 0.1774 mL | 0.3548 mL | 0.8871 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Elacridar 143664-11-3 Membrane transporter/Ion channel Neuroscience BCRP P-gp Inhibitor Multidrug resistance protein 1 cancer CD243 P-glycoprotein GG 918 Breast cancer resistance protein GW-120918 inhibit 786-O GW0918 GF-120918 ABCG2 Pgp GW 0918 MCF-7 依克立达 sunitinib ABCB1 GF 120918 GW120918 GF120918 GW 120918 MDR1 GW-0918 GG-918 GG918 Cluster of differentiation 243 inhibitor