阿帕他隆 T2480

Product Introduction
Bioactivity


英文名: Apabetalone

描述: Apabetalone (RVX000222) 是一种 BET 溴结构域抑制剂，用于研究治疗糖尿病、动脉粥样硬化和冠状动脉疾病。

细胞实验: RVX-208 is prepared in DMSO and stored, and then diluted with appropriate medium before use[2]. Huh7 cells are plated at 23,000/well in a 96 well plate in DMEM+10% FBS before allowing to grow overnight. Cells are treated with compounds for 48 h in 0.1% DMSO with or without 5 μM Actinomycin D. U937 cells are differentiated for 3 days in 60 ng/mL PMA, 32,000 cells/well in 96-well format. Cells are then treated with compound in 0.1% DMSO in RPMI media+10% FBS, and after 1 h, lipopolysaccharide is added to the cells at 1 μg/mL for 3 hours[2].

体外活性: 在AGMs中,RVX-208能够显著增加血清apoA-I和 HDL-C,同时通过多种途径增加胆固醇流出.

体内活性: 在体外实验中,RVX-208能够激活载脂蛋白AI基因表达,增加apoA-I 和 HDL-C。RVX-208能够抑制BET溴结构域蛋白,并且优先与BET蛋白质的第二溴结构域蛋白结合。

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

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 69 mg/mL (186.3 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: RVX-000222 | Inhibitor | Epigenetic Reader Domain | RVX 000222 | RVX208 | Human immunodeficiency virus | inhibit | RVX 208 | HIV | Apabetalone

相关产品: GSK217 | Piflufolastat | Eleven-Nineteen-Leukemia Protein IN-1 | Bleximenib oxalate | I-BET762 carboxylic acid | Eleven-Nineteen-Leukemia Protein IN-3 | dCBP-1 | BRM/BRG1 ATP Inhibitor-1 | PFI-1 | BRD7-IN-1

相关库: Anti-Aging Compound Library | Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | ReFRAME Related Library | Bioactive Compounds Library Max | Human Metabolite Library | Inhibitor Library | Highly Selective Inhibitor Library | Preclinical Compound Library | NO PAINS 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