Benzbromarone

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Chemical Structure| 3562-84-3 同义名 : MJ10061; Desuric; Normurat; Narcaricin; L2214-Labaz; L2214; NSC 85433
CAS号 : 3562-84-3
货号 : A218663
分子式 : C17H12Br2O3
纯度 : 98%
分子量 : 424.08
MDL号 : MFCD00078962
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
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

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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.79mL

2.36mL

1.18mL

23.58mL

4.72mL

2.36mL
参考文献

[1]Kaufmann P, Torok M, et al. Mechanisms of benzarone and benzbromarone-induced hepatic toxicity. Hepatology. 2005 Apr;41(4):925-35.

[2]Locuson CW 2nd, Wahlstrom JL, et al. A new class of CYP2C9 inhibitors: probing 2C9 specificity with high-affinity benzbromarone derivatives. Drug Metab Dispos. 2003 Jul;31(7):967-71.

[3]LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Benzbromarone. 2017 Sep 5

[4]Abdel-Razek EA, Abo-Youssef AM, Azouz AA. Benzbromarone mitigates cisplatin nephrotoxicity involving enhanced peroxisome proliferator-activated receptor-alpha (PPAR-α) expression. Life Sci. 2020 Feb 15;243:117272

[5]Sun P, Zhu JJ, Wang T, Huang Q, Zhou YR, Yu BW, Jiang HL, Wang HY. Benzbromarone aggravates hepatic steatosis in obese individuals. Biochim Biophys Acta Mol Basis Dis. 2018 Jun;1864(6 Pt A):2067-2077

[6]Roos NJ, Duthaler U, Bouitbir J, Krähenbühl S. The uricosuric benzbromarone disturbs the mitochondrial redox homeostasis and activates the NRF2 signaling pathway in HepG2 cells. Free Radic Biol Med. 2020 May 20;152:216-226

[7]Muraya N, Kadowaki D, Miyamura S, Kitamura K, Uchimura K, Narita Y, Miyamoto Y, Chuang VTG, Taguchi K, Maruyama T, Otagiri M, Hirata S. Benzbromarone Attenuates Oxidative Stress in Angiotensin II- and Salt-Induced Hypertensive Model Rats. Oxid Med Cell Longev. 2018 Jun 5;2018:7635274