Product Introduction
Bioactivity


英文名: MSU-42011

描述: MSU-42011 是一种具有口服活性的类视黄醇 X 受体 (RXR) 激动剂。MSU-42011 有效抑制iNOS，低SREBP 诱导和激活RXR 以及 p-ERK 蛋白水平的表达。MSU-42011在kras 驱动的肺癌小鼠模型中表现出抗肿瘤活性。MSU-42011可有效治疗临床前Krasdriven 肺癌且具有免疫调节活性。

体外活性: MSU-42011（300 nM；8小时）在HepG2细胞中对SREBP的诱导效果较低。[1] MSU-42011（0-5000 nM；24小时）能够在HepG2细胞中激活RXR。[1]

体内活性: MSU-42011 (25 mg/kg; oral; for 12 weeks) significantly reduced the number, size, and overall tumor burden of tumors in the A/J mouse lung cancer model. Compared with the control group, there were fewer cells with active proliferation and showed a significant decrease in p-ERK [1].MSU-42011 (25 mg/kg; oral; single dose) is most effective in reducing the number, size, and overall tumor burden of the A/J mouse lung cancer model in combination with C/P. Reduced macrophages in the lungs and increased activation markers of CD8+T cells [1].MSU42011 (100 mg/kg; PO; single dose) reduces tumor burden in a mouse lung tumor model [2].

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

溶解度: DMSO : 45 mg/mL (117.63 mM)


关键字: MSU42011 | 6((3,5ditertbutylphenyl)(isobutyl)amino)nicotinicacid | MSU 42011 | MSU-42011

相关产品: Chlojaponilactone B | Dehydroandrographolide | Catalposide | Epicatechin pentaacetate | 26-Deoxyactein | Schisandrone | Sanggenon D | Escin IIB | Neoechinulin A | Ailanthoidol

相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library