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Benzbromarone/苯溴马隆 {[allProObj[0].p_purity_real_show]}

货号:A218663 同义名: MJ10061; Desuric

Benzbromarone is a CYP2C9 inhibitor with Ki of 19.3 nM.

Benzbromarone/苯溴马隆 化学结构 CAS号:3562-84-3
Benzbromarone/苯溴马隆 化学结构
CAS号:3562-84-3
Benzbromarone/苯溴马隆 3D分子结构
CAS号:3562-84-3
Benzbromarone/苯溴马隆 化学结构 CAS号:3562-84-3
Benzbromarone/苯溴马隆 3D分子结构 CAS号:3562-84-3
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Benzbromarone/苯溴马隆 纯度/质量文件 产品仅供科研

货号:A218663 标准纯度: {[allProObj[0].p_purity_real_show]}
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Benzbromarone/苯溴马隆 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].

Benzbromarone/苯溴马隆 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

Benzbromarone/苯溴马隆 实验方案

计算器
存储液制备 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

Benzbromarone/苯溴马隆 技术信息

CAS号3562-84-3
分子式C17H12Br2O3
分子量 424.08
SMILES Code O=C(C1=CC(Br)=C(O)C(Br)=C1)C2=C(CC)OC3=CC=CC=C23
MDL No. MFCD00078962
别名 MJ10061; Desuric; Normurat; Narcaricin; L2214-Labaz; L2214; NSC 85433
运输蓝冰
InChI Key WHQCHUCQKNIQEC-UHFFFAOYSA-N
Pubchem ID 2333
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
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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