化合物NO-1886 T7832

Product Introduction
Bioactivity


英文名: Ibrolipim

描述: Ibrolipim (NO-1886) 是口服具有活力的脂蛋白脂肪酶 (LPL) 激活剂。它能够降低血浆甘油三酸酯，增加高密度脂蛋白胆固醇水平，具有肾保护和降血脂的作用。

细胞实验: Human THP-1 cells pre-incubated with ox-LDL served as foam cell models. Specific mRNA was quantified using real-time RT-PCR and protein expression using Western blotting. Cellular cholesterol handling was studied using cholesterol efflux experiments and high performance liquid chromatography assays[1]

动物实验: Animal Model: Female Sprague-Dawley rats (10-week-old; 200-260 g) with experimental ovariectomy treatment. Dosage: 100 mg/kg ? ? ??. Administration: Oral administration; daily; for 8 weeks[2]

体外活性: Ibrolipim?5 and 50 μmol/L significantly increased cholesterol efflux from THP-1 macrophage-derived foam cells to apoA-I or HDL. Moreover, it upregulated the expression of ABCA1 and ABCG1. In addition, LXRα was also upregulated by the?ibrolipim?treatment. In addition, LXRα small interfering RNA completely abolished the promotion effect that was induced by?ibrolipim[1].

体内活性: Ibrolipim (NO-1886; 100 mg/kg; oral administration; daily; for 8 weeks; female Sprague-Dawley rats) treatment decreases accumulation of visceral fat and suppresses the increase in body weight resulting from the ovariectomy. Ibrolipim decreases the respiratory quotient and increases expression of the fatty acid translocase messenger RNA (mRNA) in the liver, soleus muscle, and mesenteric fat. Ibrolipim also increases the expression of fatty acid-binding protein mRNA in the liver and soleus muscle and the expression of the uncoupling protein 3 (UCP3) mRNA in the heart, soleus muscle, and mesenteric fat, but not in the brown adipose tissue[2]

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

溶解度: DMSO : 125 mg/mL (277.01 mM)


关键字: obesity | fatty | inhibit | acid | Inhibitor | lipoprotein | lipase | Antihyperlipidemic | NO 1886 | UCP3 | NO1886 | Ibrolipim | LDL-C | LXRα | HDL-C

相关产品: NIBR-0213 | CYM50308 | PF-543 | CYM50358 | Fingolimod | S1p receptor agonist 1 | GSK2018682 | SLP9101555 | S1P1 agonist 6 | Ki16198

相关库: HIF-1 Signaling Pathway Compound Library | ReFRAME Related Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Orally Active Compound Library | NO PAINS Compound 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