依利格鲁司特 T3663

Product Introduction
Bioactivity


英文名: Eliglustat

描述: 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)。

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].

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].

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。

存储条件: 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)


关键字: inhibit | Genz-99067 | GENZ112638 | Inhibitor | Eliglustat | GENZ 112638 | Genz99067

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相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | ReFRAME Related Library | FDA-Approved & Pharmacopeia Drug Library | Clinical Compound Library | Anti-Metabolism Disease Compound Library | Inhibitor Library | EMA Approved Drug Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途