Product Introduction
Bioactivity


英文名: Benzarone

描述: Benzarone (Benzarona) 是人尿酸转运蛋白 1的有效抑制剂，IC50为 2.8 μM。它具有降低血清尿酸水平的作用。

体外活性: Studies on the action of benzarone on the metabolism of cultured arterial smooth muscle cells and arterial tissue had the following results: 1. On incubation of calf arterial tissue in the presence of 0.03--0.1 mmol/l benzarone (8--26 micrograms/ml medium) the metabolic transformation of [14C]-glucose to [14C]-lactate and 14CO2 and the incorporation of 14C radioactivity into the total lipids is not significantly altered as compared with control values. In cultured human arterial smooth muscle cells 0.03 mmol/l benzarone stimulates the incorporation of [14C]-acetate and [3H]-palmitate into the cellular lipids while the receptor mediated uptake of homologous low-density lipoproteins (LDL) by the cells and their release are not influenced. 2. In concentrations greater than 0.2 mmol/l benzarone the glucose utilisation of arterial tissue is enhanced, while the labelling of lipids, in particular the labelling of the triglyceride fraction, is depressed. Under the same conditions the protein biosynthesis and the incorporation of [14C]-acetate and [3H]-palmitate into the total lipids of cultured arterial smooth muscle cells are decreased[2].

体内活性: Rats of BD X strain and SHR/NIH Montreal Ingelheim strain (genetic hypertension) received a diet containing 3.9% cholesterol or 3.7% cholesterol plus 0.6% benzarone, respectively, and libitum for 5 or 9 months. The following chemical and ultrastructural results were obtained. 1. The cholesterol-benzarone diet causes a body weight reduction of 10%, a relative increase of serum HDL and a corresponding decrease of serum LDL and VLDL, as compared with the effects of the cholesterol diet. No differences of total serum cholesterol and serum triglycerides between the two groups were observed. 2. The aorta of cholesterol fed animals shows a slight but statistically not significant increase of total cholesterol content. 3. No differences in the composition of connective tissue components (collagen, elastin, uronic acid content) between the cholesterol fed animals and a control group on normal diet could be detected. 4. Electron micrographs of several vessel wall areas from cholesterol fed hypertensive animals revealed fibrosis, necrosis of media muscle cells and an increase of matrix vesicles. Severe damages were found in coronary arteries and in the caudal arteries. 5. Cholesterol feeding of hypertensive rats increases the cholesterol content of liver 10fold and the triglycerides content 3fold as compared with liver lipids of control rats. Benzarone application to cholesterol fed rats effects a statistically significant decrease of liver cholesterol and triglycerides[3].

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

溶解度: DMSO : 55 mg/ml (206.54 mM)


关键字: Inhibitor | URAT1 | uric acid | inhibit | Benzarone | SLC22A12 | Urate transporter 1 | Fragivix | hURAT1

相关产品: Lesinurad | Verinurad | Puliginurad | Lingdolinurad | Dotinurad | Indican | Fraxin | URAT1 inhibitor 7 | URAT1 inhibitor 1

相关库: Ion Channel Inhibitor Library | ReFRAME Related Library | Anti-Cancer Compound Library | Drug-induced Liver Injury (DILI) Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Human Metabolite Library | Inhibitor Library | Bioactive Compound Library