Benzarone NEW
Price | $39 |
Package | 500mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-06 |
Product Details
Product Name: Benzarone | CAS No.: 1477-19-6 |
Purity: 99.33% | Supply Ability: 10g |
Release date: 2024/11/06 |
Product Introduction
Bioactivity
名稱 | Benzarone |
描述 | Benzarone (Benzarona) is a potent inhibitor of human uric acid transporter 1 (URAT1, IC50 = 2.8 μM in oocyte). Benzarone lowers the level of uric acid serum. |
體外活性 | 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]. |
體內(nèi)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]. |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 55 mg/ml (206.54 mM) |
關(guān)鍵字 | Inhibitor | URAT1 | uric acid | inhibit | Benzarone | SLC22A12 | Urate transporter 1 | Fragivix | hURAT1 |
相關(guān)產(chǎn)品 | Fraxin | Indican | Verinurad | Puliginurad | URAT1 inhibitor 7 | Lesinurad | Epaminurad HCl | Lingdolinurad | URAT1 inhibitor 1 | Dotinurad |
相關(guān)庫 | 經(jīng)典已知活性庫 | 膜蛋白靶向化合物庫 | ReFRAME 相關(guān)化合物庫 | 肝臟毒性化合物庫 | 抑制劑庫 | 已知活性化合物庫 | 離子通道庫 | 抗癌化合物庫 | 人代謝物化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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