價格 | ¥192 | ¥389 | ¥626 |
包裝 | 1mg | 5mg | 10mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-12-02 |
中文名稱:依克立達 | 英文名稱:Elacridar |
CAS:143664-11-3 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 99.62% | 產(chǎn)品類別: 抑制劑 |
貨號: T2657 |
名稱 | Elacridar |
描述 | Elacridar (GG918) is a potent inhibitor of P-glycoprotein and BCRP. |
細胞實驗 | 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) |
激酶實驗 | 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. |
體外活性 | 方法: MCF-7、Caki-1 和 786-O 細胞系用Elacridar (GG918)(5μM,24小時),制備細胞裂解物并裝入每個孔中,通過免疫印跡確定蛋白質(zhì)表達,檢測 β-肌動蛋白的表達以標(biāo)準(zhǔn)化總蛋白質(zhì)負載。 結(jié)果:Elacridar (GG918)影響MCF-7和786-O細胞系中的P-糖蛋白和ABCG2蛋白表達水平;影響Tc-MIBI在MCF-7和786-O細胞中的細胞內(nèi)積累。[2] |
體內(nèi)活性 | 方法:Elacridar (GG918)以三種不同的給藥方式(2.5mg/kg,靜脈注射;100mg/kg,腹腔注射;100mg/kg,口服)給FVB 野生型小鼠,研究Elacridar (GG918) 在血漿和大腦中的藥代動力學(xué)參數(shù)。 結(jié)果:Elacridar (GG918)在三種給藥方式中血漿和大腦中的藥代動力學(xué)參數(shù)不同:靜脈注射給藥血漿中半衰期為 4.4 小時,腦中為 1.5 小時,Kp值為0.82;腹腔注射血漿中半衰期為 4.3 小時,腦中為 9.2小時,Kp值為0.48;腹腔注射血漿中半衰期為 20 小時,腦中為 16小時,Kp值為4.31。[1] |
存儲條件 | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 7.86 mg/mL (13.94 mM) |
關(guān)鍵字 | Inhibitor | Multidrug resistance protein 1 | cancer | CD243 | P-glycoprotein | GG 918 | Breast cancer resistance protein | GW-120918 | P-gp | inhibit | 786-O | GF-120918 | ABCG2 | Pgp | BCRP | GW 0918 | MCF-7 | sunitinib | ABCB1 | GF 120918 | GW 120918 | MDR1 | GW-0918 | GG-918 | Cluster of differentiation 243 | Elacridar |
相關(guān)產(chǎn)品 | Cinchonine | Piperine | P-gp inhibitor 1 | Glibenclamide | Verapamil hydrochloride | Atazanavir | Selamectin | Polyoxyethylene stearate | Atazanavir sulfate | Muscone | Encequidar mesylate | Verapamil |
相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 抗癌活性化合物庫 | 已知活性化合物庫 | 神經(jīng)信號分子庫 | 離子通道庫 | 膜蛋白靶向化合物庫 | 藥物功能重定位化合物庫 | 抗癌臨床化合物庫 | 抗癌藥物庫 |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 566.2651萬人民幣 |
員工人數(shù) | 100-500人 | 年營業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 化學(xué)試劑,生物活性小分子 | 經(jīng)營模式 | 貿(mào)易,試劑,定制,服務(wù) |
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