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  • 產(chǎn)品名稱: Eliglustat 依利格魯司特
  • 產(chǎn)品貨號(hào): CST3663
  • 貨期: 現(xiàn)貨
  • 價(jià)格與訂購(gòu): 1280
  • 數(shù)量:
    庫(kù)存: 5
  • 規(guī)格: 100mg
  • 產(chǎn)品信息
  • 如何訂購(gòu)
    產(chǎn)品描述
    Eliglustat is an oral inhibitor of glucosylceramide synthase which is used in the therapy of type 1 Gaucher disease.
    體外活性
    Eliglustat Tartrate嚙齒類(lèi)動(dòng)物體內(nèi)快速代謝,其體內(nèi)半衰期在15-45分鐘.對(duì)正常小鼠、大鼠、狗中通過(guò)靜脈注射和口服途徑給藥(Eliglustat Tartrate),脾臟、腎臟和肝臟中葡糖神經(jīng)酰胺的含量顯著下降.
    體內(nèi)活性
    Eliglustat tartrate是葡萄糖神經(jīng)酰胺合成酶的抑制劑,對(duì)該酶的抑制作用高度特異,對(duì)其他多種糖苷酶的抑制作用有限甚至沒(méi)有抑制活性。
    激酶實(shí)驗(yàn)
    Smo-binding assays are conducted with BODIPY-cyclopamine and Smo-overexpressing HEK 293T cells, using a CMVpromoter-based SV40 origin-containing expression construct for Smo-Myc3 (murine Smo containing three consecutive Myc epitopes at the C terminus). HEK 293T cells are seeded into eight-well chambered coverslips (80,000 cells/well) and cultured in DMEM containing 10% FBS, 100 U/mL penicillin, and 0.1 mg/mL streptomycin. The cells are cultured until they reached 55 to 65% confluency (14-18 h), after which they are transfected with the Smo-Myc3 expression construct and Transit-LT1. Twenty-four hours after transfection, the cells are washed with PBS and cultured in DMEM containing 0.5% FBS, 5 nM BODIPY-cyclopamine, and various concentrations of either cyclopamine or individual HPIs. After 30 min, 10 μM Hoescht 33342 is added to each well, and the HPIs are incubated with the cells for an additional 30 min. The cells are then washed two times with PBS buffer, once with phenol red-free DMEM containing 0.5% FBS, and immediately imaged using a DMI6000B compound microscope. Images are background-substracted using ImageJ software with a rolling ball size of 75 pixels, and BODIPY-cyclopamine intensity is then determined using Metamorph software. Circular regions with a diameter of 300 pixels are placed over regions containing uniformly confluent cells, and the pixel intensities of approximately 20 regions from four independent images is used to determine the average BODIPY-cyclopamine levels for each experimental condition[1].
    細(xì)胞實(shí)驗(yàn)
    The inhibitory activity of Genz-112638 is determined indirectly by measuring its effect on the cell surface levels of the gangliosides GM1 and GM3 on either K562 or B16/F10 cells. GM1 levels on the K562 cells are determined by incubating the cells with increasing amounts of Genz-112638 (0.6-1000 nM) for 72 h after which the cells are harvested and stained using 10 μg of recombinant cholera toxin-FITC in 100 μL phosphate buffered saline (PBS) containing 0.5% bovine serum albumin (BSA) for 30 min on ice. Cells are ished, resuspended in PBS containing 0.5% BSA and the fluorescence quantitated[1].
    分子式
    C23H36N2O4
    分子量
    404.551 
    別名
    依利格魯司特;GENZ-112638;Genz 99067
    參考文獻(xiàn)
    [1]Shayman JA. Drugs Future. 2010, 35(8):613-620.
    [2]Nelson S. Yew, et al. PLoS One. 2010, 5(6):e11239.icon
    儲(chǔ)存和溶解度
    DMSO:74 mg/mL (182.9 mM)
    H2O:<1 mg/mL
    Ethanol:74 mg/mL (182.9 mM)
    Powder: -20°C for 3 years
    In solvent: -80°C for 2 years
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    Note
    For Research Use Only.