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Eliglustat

Eliglustat

产品编号 T3663   CAS 491833-29-5
别名: GENZ-112638, Genz 99067, 依利格鲁司特

Eliglustat (Genz 99067) 是一种高效的、特异性的、有口服活性的葡糖脑苷脂合成酶抑制剂(IC50:24 nM)。

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Eliglustat Chemical Structure
Eliglustat, CAS 491833-29-5
规格 价格/CNY 货期 数量
1 mg ¥ 413 现货
2 mg ¥ 588 现货
5 mg ¥ 872 现货
10 mg ¥ 1,280 现货
25 mg ¥ 2,570 现货
50 mg ¥ 3,960 现货
100 mg ¥ 5,660 现货
500 mg ¥ 11,700 现货
1 mL * 10 mM (in DMSO) ¥ 775 现货
其他形式的 Eliglustat:
产品目录号及名称: Eliglustat (T3663)
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纯度: 99.71%
纯度: 99%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Eliglustat (Genz 99067) is an oral inhibitor of glucosylceramide synthase which is used in the therapy of type 1 Gaucher disease.
靶点活性 glucosylceramide synthase:20 nM
体外活性 Eliglustat Tartrate啮齿类动物体内快速代谢,其体内半衰期在15-45分钟.对正常小鼠、大鼠、狗中通过静脉注射和口服途径给药(Eliglustat Tartrate),脾脏、肾脏和肝脏中葡糖神经酰胺的含量显著下降.
体内活性 Eliglustat tartrate是葡萄糖神经酰胺合成酶的抑制剂,对该酶的抑制作用高度特异,对其他多种糖苷酶的抑制作用有限甚至没有抑制活性。
激酶实验 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].
细胞实验 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].
别名 GENZ-112638, Genz 99067, 依利格鲁司特
分子量 404.54
分子式 C23H36N2O4
CAS No. 491833-29-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 74 mg/mL (182.9 mM)

DMSO: 74 mg/mL (182.9 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.4719 mL 12.3597 mL 24.7194 mL 61.7986 mL
5 mM 0.4944 mL 2.4719 mL 4.9439 mL 12.3597 mL
10 mM 0.2472 mL 1.236 mL 2.4719 mL 6.1799 mL
20 mM 0.1236 mL 0.618 mL 1.236 mL 3.0899 mL
50 mM 0.0494 mL 0.2472 mL 0.4944 mL 1.236 mL
100 mM 0.0247 mL 0.1236 mL 0.2472 mL 0.618 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Shayman JA. Drugs Future. 2010, 35(8):613-620. 2. Nelson S. Yew, et al. PLoS One. 2010, 5(6):e11239.
CBHcy Risedronic Acid Serotonin OU749 Miglustat hydrochloride GGTI-2133 Ibandronate sodium Testosterone propionate

相关化合物库

该产品包含在如下化合物库中:
药物功能重定位化合物库 临床期小分子药物库 肝脏毒性化合物库 抗COVID-19化合物库 人代谢物化合物库 口服活性化合物库 代谢化合物库 已知活性化合物库 FDA上市及药典收录分子库 NO PAINS 化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

Eliglustat 491833-29-5 Metabolism Transferase inhibit GENZ-112638 Genz-99067 GENZ112638 Inhibitor Genz 99067 GENZ 112638 Genz99067 依利格鲁司特 inhibitor

 

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