Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ARN5187 是一种亲溶酶体化合物,是 REV-ERBβ的配体。ARN5187抑制 REV-ERB 介导的转录调控和细胞自噬。ARN5187 显示出溶酶体效力和细胞毒性,可诱导细胞凋亡 (apoptosis)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | ARN5187 is a lysosomal compound, REV-ERB β Ligand. ARN5187 inhibits REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomal efficacy and cytotoxicity, and can induce apoptosis. |
体外活性 | ARN5187 (compound 1) (0-100 μM; 48 h) shows cytotoxicity with EC 50 of 23.5 μM in BT-474 cells and IC 50 of 30.14 μM, >100 μM for BT-474 and HMEC cells, respectively [1] [2]. ARN5187 (0-100 μM) activates the RevRE reporter in a concentration-dependent manner in HEK-293 cells [1]. ARN5187 (25, 50 μM) is a lysosomotropic-independent REV-ERB antagonistic activity [1]. ARN5187 (50 μM; 24 h) shows autophagy inhibition [1]. ARN5187 (50 μM; 2, 8, 24 h) effects autophagy formation and maturation [1]. Cell Cytotoxicity Assay [1] Cell Line: BT-474 cells Concentration: 0-100 μM Incubation Time: 48 h Result: Showed cytotoxicity with EC 50 of 23.5 μM. RT-PCR [1] Cell Line: BT-474 cells Concentration: 25, 50 μM Incubation Time: Result: Significantly enhanced the expression of BMAL1, PER1 and PEPCK in a dose-dependent manner. Western Blot Analysis [1] Cell Line: BT-474 cells Concentration: 50 μM Incubation Time: 24 h Result: Significantly increased the expression of α-LC3-II, α-p62, α-Cleaved PARP. |
分子量 | 397.53 |
分子式 | C24H32FN3O |
CAS No. | 1287451-26-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
ARN5187 1287451-26-6 Inhibitor inhibitor inhibit