產品屬性：

Cas No.: 1477-19-6

別名: N/A

化學名: N/A

分子式: C17H14O3

分子量: 266.3

溶解度: DMF: 30 mg/ml,DMSO: 10 mg/ml,Ethanol: 10 mg/ml

儲存條件: -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

產品描述：

Benzarone is an active metabolite of the urate anion transporter 1 (URAT1) inhibitor benzbromarone .1,2 It inhibits URAT1 in Xenopus oocytes expressing the human enzyme (IC50 = 2.8 μM).2 Benzarone 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.3 It uncouples oxidative phosphorylation in isolated rat liver mitochondria and induces apoptosis and necrosis in isolated rat hepatocytes.4 Benzarone (25 μg/g) reduces tumor growth in an A-673 Ewing sarcoma mouse xenograft model.51.Stüber, W., and M?ller, 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., T?r?k, M., H?nni, 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)
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