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CAS No.: 3562-84-3

苯溴马隆 Catalog No. CSN16313

Synonyms: 苯溴马隆

Benzbromarone is a CYP2C9 inhibitor with Ki of 19.3 nM.

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生物活性

描述Benzbromarone is a highly effective and well tolerated non-competitive inhibitor of xanthine oxidase, used as an uricosuric agent, used in the treatment of gout^[3]. Benzbromarone retarded apoptosis associated with reducing the pro-apoptotic (Bax) and enhancing the anti-apoptotic (Bcl-2) protein expressions^[4]. Importantly, prolonged treatment of benzbromarone significantly increased cell apoptosis in HepG2 cells in the presence of high FFAs(free fatty acids). In addition, in benzbromarone-treated hyperuricemic patients, serum transaminase levels were positively correlated with patients' obesity level^[5]. Benzbromarone increased mitochondrial O2•- accumulation and activates the NRF2 signaling pathway in HepG2 cells, thereby strengthening the cytosolic and mitochondrial antioxidative defense^[6]. Benzbromarone has a direct antioxidant effect in vivo and great potential to prevent CVD (cardiovascular disease) and CKD (chronic kidney disease) ^[7].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03185793	Hyperuricemia	Phase 2	Recruiting	April 30, 2018	China, Shanghai ... more >> Jiangsu Hengrui Medicine Co., Ltd. Recruiting Shanghai, Shanghai, China, 200127 Contact: Chunde Bao, Master 8613601689747 baochunde_1678@126.com Collapse <<
NCT02317861	Gout and Asymptomatic Hyperuri... more >>cemia Collapse <<	Phase 1 Phase 2	Completed	-	Japan ... more >> Research Site Fukuoka-shi, Japan Collapse <<
NCT03534037	Hyperuricemia ... more >> Metabolic Syndrome Left Ventricular Diastolic Dysfunction Collapse <<	Phase 4	Active, not recruiting	March 2020	Taiwan ... more >> Tri-service General Hospital, songshan branch Taipei, Songshan Dist., Taiwan, 105 Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3580 mL
- 11.7901 mL
- 23.5803 mL
- 5 mM
- 0.4716 mL
- 2.3580 mL
- 4.7161 mL
- 10 mM
- 0.2358 mL
- 1.1790 mL
- 2.3580 mL

技术信息

CAS号

3562-84-3

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H12Br2O3

运输

蓝冰

分子量

424.08

别名

苯溴马隆

溶解度

DMSO	440.0 mg/mL (1037.5 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	8 mg/mL	clear
PO	0.5% CMC-Na	60 mg/mL	suspension

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03185793	Hyperuricemia	Phase 2	Recruiting	April 30, 2018	China, Shanghai ... more >> Jiangsu Hengrui Medicine Co., Ltd. Recruiting Shanghai, Shanghai, China, 200127 Contact: Chunde Bao, Master 8613601689747 baochunde_1678@126.com Collapse <<
NCT02317861	Gout and Asymptomatic Hyperuri... more >>cemia Collapse <<	Phase 1 Phase 2	Completed	-	Japan ... more >> Research Site Fukuoka-shi, Japan Collapse <<
NCT03534037	Hyperuricemia ... more >> Metabolic Syndrome Left Ventricular Diastolic Dysfunction Collapse <<	Phase 4	Active, not recruiting	March 2020	Taiwan ... more >> Tri-service General Hospital, songshan branch Taipei, Songshan Dist., Taiwan, 105 Collapse <<
NCT03691688	-	-	Recruiting	March 1, 2022	China, Shanghai ... more >> Shanghai Zhongshan Hospital Recruiting Shanghai, Shanghai, China, 200032 Contact: Shalaimaiti Shali, MD 86+13761553110 shali@zs-hospital.sh.cn Contact: Yuxiang Dai, MD,PhD +86-13818988550 dai.yuxiang@zs-hospital.sh.cn Principal Investigator: Junbo Ge, Professor Collapse <<
NCT03100318	Hyperuricemia With or Without ... more >>Gout Collapse <<	Phase 3	Completed	-	Japan ... more >> Tokyo Tokyo, Japan Collapse <<
NCT00422318	Heart Failure ... more >> Hyperuricemia Collapse <<	Phase 4	Completed	-	Japan ... more >> Tottori University Hospital Yonago, Japan, 683-8504 Collapse <<
NCT02944214	Chronic Kidney Disease ... more >> Hyperuricemia Abnormal Renal Function Collapse <<	Not Applicable	Not yet recruiting	December 2019	China, Shanghai ... more >> Department of Nephrology & Rheumatology, Shanghai Tenth People's Hospital Not yet recruiting Shanghai, Shanghai, China, 200072 Contact: Ai Peng, MD, PhD pengai@tongji.edu.cn Collapse <<
NCT02338323	Chronic Kidney Disease ... more >> Hyperuricemia Abnormal Renal Function Collapse <<	Not Applicable	Unknown	December 2018	China, Shanghai ... more >> Department of Nephrology & Rheumatology, Shanghai Tenth People's Hospital Recruiting Shanghai, Shanghai, China, 200072 Contact: Ai Peng, MD, PhD pengai@tongji.edu.cn Contact: Ling Wang, MD, PhD nowax@126.com Sub-Investigator: Ling Wang, MD, PhD Collapse <<
NCT02790450	Idiopathic Pulmonary Arterial ... more >>Hypertension Collapse <<	Phase 2	Completed	-	Austria ... more >> Medical University of Graz Graz, Austria, 8036 Collapse <<

苯溴马隆 Catalog No. CSN16313

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