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抑制剂描述:

产品名称:Benzbromarone

产品别名:见爱必信官网

英文别名:Benzbromarone

靶点:P450

CAS:3562-84-3

纯度:99%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.

溶解性:Ethanol :9 mg/mL (21.22 mM)
DMSO :79 mg/mL (186.3 mM)

体外研究:

Benzbromarone (20 μM) decreases mitochondrial membrane potential by 81% in isolated rat hepatocytes. Benzbromarone decreases state 3 oxidation and respiratory control ratios for L-glutamate with IC50 Benzbromarone significantly reduces the oxypurinol uptake at a concentration as low as 10 nM and completely blocks it at 1 μM. Benzbromarone (1 μM) uptakes the typical substrate of OCTN1 (tetraethylammonium) and OCTN2 (carnitine) in the HEK293 cells expressed with human OCTN1 by 96.7% and 111% of control, respectively. Benzbromarone completely inhibits urate uptake at 50 μM in URAT1-expressing oocytes, with IC50 of less than 0.1 μM. Benzbromarone activates through sequential hydroxylation of the benzofuran ring to a catechol, which can then be further oxidized to a reactive quinone intermediate capable of adducting protein.

体内研究:

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