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Benzarone

产品编号 T20545 CAS 1477-19-6

别名: Benzarona, Vasoc, 苯扎隆, Venagil, Benzaronum

Benzarone (Benzarona) 是人尿酸转运蛋白 1的有效抑制剂，IC50为 2.8 μM。它具有降低血清尿酸水平的作用。

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Benzarone, CAS 1477-19-6

规格	价格/CNY	货期
500 mg	￥ 282	现货
1 g	￥ 345	现货
1 mL * 10 mM (in DMSO)	￥ 175	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Benzarone (Benzarona) is a potent inhibitor of human uric acid transporter 1 (URAT1, IC50 = 2.8 μM in oocyte). Benzarone lowers the level of uric acid serum.
靶点活性	URAT1:2.8 μM(oocyte)
体外活性	Studies on the action of benzarone on the metabolism of cultured arterial smooth muscle cells and arterial tissue had the following results: 1. On incubation of calf arterial tissue in the presence of 0.03--0.1 mmol/l benzarone (8--26 micrograms/ml medium) the metabolic transformation of [14C]-glucose to [14C]-lactate and 14CO2 and the incorporation of 14C radioactivity into the total lipids is not significantly altered as compared with control values. In cultured human arterial smooth muscle cells 0.03 mmol/l benzarone stimulates the incorporation of [14C]-acetate and [3H]-palmitate into the cellular lipids while the receptor mediated uptake of homologous low-density lipoproteins (LDL) by the cells and their release are not influenced. 2. In concentrations greater than 0.2 mmol/l benzarone the glucose utilisation of arterial tissue is enhanced, while the labelling of lipids, in particular the labelling of the triglyceride fraction, is depressed. Under the same conditions the protein biosynthesis and the incorporation of [14C]-acetate and [3H]-palmitate into the total lipids of cultured arterial smooth muscle cells are decreased[2].
体内活性	Rats of BD X strain and SHR/NIH Montreal Ingelheim strain (genetic hypertension) received a diet containing 3.9% cholesterol or 3.7% cholesterol plus 0.6% benzarone, respectively, and libitum for 5 or 9 months. The following chemical and ultrastructural results were obtained. 1. The cholesterol-benzarone diet causes a body weight reduction of 10%, a relative increase of serum HDL and a corresponding decrease of serum LDL and VLDL, as compared with the effects of the cholesterol diet. No differences of total serum cholesterol and serum triglycerides between the two groups were observed. 2. The aorta of cholesterol fed animals shows a slight but statistically not significant increase of total cholesterol content. 3. No differences in the composition of connective tissue components (collagen, elastin, uronic acid content) between the cholesterol fed animals and a control group on normal diet could be detected. 4. Electron micrographs of several vessel wall areas from cholesterol fed hypertensive animals revealed fibrosis, necrosis of media muscle cells and an increase of matrix vesicles. Severe damages were found in coronary arteries and in the caudal arteries. 5. Cholesterol feeding of hypertensive rats increases the cholesterol content of liver 10fold and the triglycerides content 3fold as compared with liver lipids of control rats. Benzarone application to cholesterol fed rats effects a statistically significant decrease of liver cholesterol and triglycerides[3].

别名	Benzarona, Vasoc, 苯扎隆, Venagil, Benzaronum
分子量	266.29
分子式	C17H14O3
CAS No.	1477-19-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 55 mg/ml (206.54 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.7553 mL	18.7765 mL	37.553 mL	93.8826 mL
	5 mM	0.7511 mL	3.7553 mL	7.5106 mL	18.7765 mL
	10 mM	0.3755 mL	1.8777 mL	3.7553 mL	9.3883 mL
	20 mM	0.1878 mL	0.9388 mL	1.8777 mL	4.6941 mL
	50 mM	0.0751 mL	0.3755 mL	0.7511 mL	1.8777 mL
	100 mM	0.0376 mL	0.1878 mL	0.3755 mL	0.9388 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Kaufmann P, Török M, Hänni A, Roberts P, Gasser R, Krähenbühl S. Mechanisms of benzarone and benzbromarone-induced hepatic toxicity. Hepatology. 2005 Apr;41(4):925-35. PubMed PMID: 15799034. 2. de Vries JX, Walter-Sack I, van de Loo A, Kocher J. Determination of benzarone in human plasma and urine by high-performance liquid chromatography and gas chromatography-mass spectrometry. Identification of the conjugates. J Chromatogr. 1986 Oct 31;382:167-74. PubMed PMID: 3782383. 3. Knehr HE, Betz E. [Effect of benzarone on the oxygen consumption and the mechanical activity of vascular smooth muscle]. Arzneimittelforschung. 1983;33(2):211-4. German. PubMed PMID: 6682659. 4. Wood SG, John BA, Chasseaud LF, Bonn R, Grote H, Sandrock K, Darragh A, Lambe RF. Metabolic fate of the thrombolytic agent benzarone in man: comparison with the rat and dog. Xenobiotica. 1987 Jul;17(7):881-96. PubMed PMID: 3660858.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Benzarone 1477-19-6 Membrane transporter/Ion channel OAT Benzarona Inhibitor URAT1 uric acid inhibit SLC22A12 Urate transporter 1 Vasoc 苯扎隆 Venagil Fragivix Benzaronum hURAT1 inhibitor

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Benzarone

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords