您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Benzarone
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Benzarone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Benzarone图片
CAS NO:1477-19-6
包装与价格:
包装价格(元)
1 g电议
5 g电议
10 g电议

产品介绍
Benzarone (Fragivix) 是一种有效的人类尿酸转运蛋白 1 (hURAT1) 抑制剂,在卵母细胞中的 IC50 为 2.8 μM。
Cas No.1477-19-6
别名苯扎隆,Fragivix
Canonical SMILESO=C(C1=C(CC)OC2=CC=CC=C12)C3=CC=C(C=C3)O
分子式C17H14O3
分子量266.3
溶解度DMF: 30 mg/ml,DMSO: 10 mg/ml,Ethanol: 10 mg/ml
储存条件-20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Benzarone is an active metabolite of the urate anion transporter 1 (URAT1) inhibitor benzbromarone .1,2It inhibits URAT1 inXenopusoocytes expressing the human enzyme (IC50= 2.8 µM).2Benzarone also inhibits the tyrosine phosphatase activity of eyes absent homolog 3 (EYA3; IC50= 17.5 µM), as well as reduces the proliferation and migration of human umbilical vein endothelial cells (HUVECs) when used at a concentration of 7.5 µM.3It uncouples oxidative phosphorylation in isolated rat liver mitochondria and induces apoptosis and necrosis in isolated rat hepatocytes.4Benzarone (25 µg/g) reduces tumor growth in an A-673 Ewing sarcoma mouse xenograft model.5

1.StÜber, W., and MÖller, H.Determination of benzbromarone, bromobenzarone and benzarone in plasma by gas chromatography—mass spectrometryJ. Chromatogr. B Biomed. Sci. Appl.224(2)327-331(1981) 2.Wempe, M.F., Jutabha, P., Quade, B., et al.Developing potent human uric acid transporter 1 (hURAT1) inhibitorsJ. Med. Chem.54(8)2701-2713(2011) 3.Pandey, R.N., Wang, T.S., Tadjuidje, E., et al.Structure-activity relationships of benzbromarone metabolites and derivatives as EYA inhibitory anti-angiogenic agentsPLoS One8(12)e84582(2013) 4.Kaufmann, P., TÖrÖk, M., HÄnni, A., et al.Mechanisms of benzarone and benzbromarone-induced hepatic toxicityHepatology41(4)925-935(2005) 5.Wang, Y., Pandey, R.N., Roychoudhury, K., et al.Targeting EYA3 in ewing sarcoma retards tumor growth and angiogenesisMol. Cancer Ther.20(5)803-815(2021)