Benzbromarone

製品コードS4221 バッチS422101

印刷

化学情報

Chemical Structure Synonyms Desuric Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H12Br2O3
分子量 424.08 CAS No. 3562-84-3
Solubility (25°C)* 体外 DMSO 85 mg/mL (200.43 mM)
Ethanol 9 mg/mL (21.22 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO Corn oil
10.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Benzbromarone(Desuric) is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM.
in vitro

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. [2] 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. [3] Benzbromarone completely inhibits urate uptake at 50 μM in URAT1-expressing oocytes, with IC50 of less than 0.1 μM. [4] 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. [5]

プロトコル(参考用のみ)

キナーゼアッセイ Enzyme Incubations
Incubations are carried out in duplicate or triplicate. Dilauroylphosphatidylcholine in chloroform is rotovapped, hydrated in 50 mM KPi buffer overnight at 4℃, and extruded through a 100-nm pore membrane (Avanti Polar Lipids Inc.) to make unilamellar vesicles. CYP2C9 is added to 2 Eq of reductase. After 30 min on ice, 0.2 μg of dilauroylphosphatidylcholine is added per picomole of 2C9. Cyt b5 (1 Eq) finished the enzyme mixture. Stocks of Benzbromarone are prepared in water with 1 Eq of KOH and gentle heat. The methanol volume does not exceed 0.1% of the total incubation volume. Reconstituted 2C9 (20 pmol) is incubated with 1000 U of catalase and (S)-warfarin at concentrations between 2.0 and 40 μM at three concentrations of inhibitor (below, at, or above the Ki) in 1 mL of 50 mM KPi, pH 7.4, in a shaking incubator at 37℃. NADPH (1 μmol) is used to initiate the reaction and 0.6 mL of acetone to quench it after 30 to 40 min.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Drug repositioning as a therapeutic strategy for neurodegenerations associated with OPA1 mutations [ Hum Mol Genet, 2020, ddaa244] PubMed: 33231680

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。