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Benzbromarone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Benzbromarone图片
CAS NO:3562-84-3
规格:≥98%
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)424.08
FormulaC17H12Br2O3
CAS No.3562-84-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 85 mg/mL (200.4 mM)
Water: <1 mg/mL
Ethanol: 9 mg/mL (21.2 mM)
Other info

Chemical Name: (3,5-dibromo-4-hydroxyphenyl)(2-ethylbenzofuran-3-yl)methanone

InChi Key: WHQCHUCQKNIQEC-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H12Br2O3/c1-2-13-15(10-5-3-4-6-14(10)22-13)16(20)9-7-11(18)17(21)12(19)8-9/h3-8,21H,2H2,1H3

SMILES Code: O=C(C1=CC(Br)=C(O)C(Br)=C1)C2=C(CC)OC3=CC=CC=C23

SynonymsL2214; MJ10061; L 2214; MJ-10061; L-2214; L2214-Labaz; Narcaricin; Normurat; Benzbromarone; MJ 10061;
实验参考方法
In Vitro

In vitro activity: 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 < 1 μM in isolated rat liver mitochondria. Benzbromarone (50 μM) uncouples oxidative phosphorylation and increases oxygen consumption by hepatocytes starting at 10 μM in isolated rat hepatocytes. Benzbromarone also inhibits the formation of acid-soluble β-oxidation products in a dose-dependent manner with IC50 of 2 μM. Benzbromarone (100 μM) inhibits the electron transport chain and are uncouplers of oxidative phosphorylation in isolated rat liver mitochondria. Benzbromarone (1 μM) leads to concentration-dependent increasion of ROS production in HepG2 cells. Benzbromarone (100 μM) leads to a significant increase in mitochondrial size of isolated rat liver mitochondria. Benzbromarone is associated with leakage of cytochrome c into the cytoplasm of HepG2 cells. Benzbromarone (100 μM) results in the proportion of apoptotic cells of 11% in rat hepatocytes. 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. [1,2]

In VivoThe in vivo urate lowering effects of JNS4 were evaluated with Benzbromarone (BM) as positive control. Potassium oxonate and hypoxanthine were used for inducing hyperuricemia in KM mice, lesinurad was used as another positive drug. As shown in Fig. 7, the serum urate levels of model group (950.4 μM) were significantly increased (P < 0.001) compared with control group (216.4 μM); while JNS4 dose-dependently lowered the serum urate levels at doses of 1, 2, 4 mg/kg (p.o.), as compared to the model group. JNS4 demonstrated better urate lowering effects than that of BM and lesinurad at the dose of 2 mg/kg, and 2 mg/kg of JNS4 achieved similar efficacy to that of 4 mg/kg of BM. [3]
Animal modelHyperuricemia model in KM mice
Formulation & Dosage4 mg/kg of BM; PO
References

[1] Drug Metab Dispos. 2003 Jul;31(7):967-71;

[2] Hepatology. 2005 Apr;41(4):925-35.

[3] Eur J Med Chem. 2022 242, 114682.