Febuxostat

製品コードS1547 バッチS154702

印刷

化学情報

Chemical Structure Synonyms TMX 67, TEI-6720 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H16N2O3S
分子量 316.37 CAS No. 144060-53-7
Solubility (25°C)* 体外 DMSO 63 mg/mL (199.13 mM)
Water Insoluble
Ethanol Insoluble
* <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 Febuxostat (TMX 67, TEI-6720) is a selective xanthine oxidase inhibitor with Ki of 0.6 nM.
in vitro Febuxostat displays potent mixed-type inhibition of the activity of purified bovine milk xanthine oxidase, with Ki and Ki' values of 0.6 nM and 3.1 nM respectively, indicating inhibition of both the oxidized and reduced forms of xanthine oxidase. [2]
in vivo Febuxostat (5–6 mg/kg/day) combined with fructose significantly lowers blood pressure, UA, triglycerides, and insulin in rats compared with fructose alone. Febuxostat (5–6 mg/kg/day) combined with fructose also reduces glomerular pressure, renal vasoconstriction, and afferent arteriolar area in rats compared with fructose alone. [2] Febuxostat prevents hyperuricemia in 5/6 nephrectomy (5/6 Nx)+oxonic acid (OA)+Febuxostat(Fx) rats and ameliorates proteinuria, preserves renal function and prevents glomerular hypertension in both 5/6 nephrectomy (5/6 Nx)+vehicle (V)+Febuxostat(Fx) and 5/6 nephrectomy (5/6 Nx)+oxonic acid (OA)+Febuxostat(Fx) groups. [3] Febuxostat (5 mg/kg/d by gavage for 8 days) treatment after transverse aortic constriction (TAC) attenuates the TAC-induced left ventricular (LV) hypertrophy and dysfunction. Febuxostat blunts the TAC-induced increases in nitrotyrosine (indicating reduced myocardial oxidative stress), p-Erk(Thr202/Tyr204), and p-mTOR(Ser2488), with no effect on total Erk or total mTOR. [4] Febuxostat significantly suppresses oxonic acid activity, and thereby reduces oxidative stress in Sprague-Dawley rats with right nephrectomy and left renal I/R injury, as assessed by nitrotyrosine, thiobarbituric acid-reactive substances (TBARS) and urine 8-isoprostane. Febuxostat also reduces the induction of endoplasmic reticulum (ER) stress in Sprague-Dawley rats with right nephrectomy and left renal I/R injury, as assessed by GRP-78, ATF4, and CHOP. [5]

プロトコル(参考用のみ)

カスタマーフィードバック

, , Free Radical Biology and Medicine, 2015, 159-166.

, , Br J Pharmacol, 2016, 173(14):2290-302.

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：

Febuxostat increases ventricular arrhythmogenesis through calcium handling dysregulation in human induced pluripotent stem cell-derived cardiomyocytes [ Toxicol Sci, 2022, kfac073] PubMed: 35866629
Metabolic Changes Are Associated with Melphalan Resistance in Multiple Myeloma [ J Proteome Res, 2021, 20(6):3134-3149] PubMed: 34014671
Identification of Modulators of HIV-1 Proviral Transcription from a Library of FDA-Approved Pharmaceuticals [ Viruses, 2020, 12(10)E1067] PubMed: 32977702
Ripk3 promotes ER stress-induced necroptosis in cardiac IR injury: A mechanism involving calcium overload/XO/ROS/mPTP pathway. [ Redox Biol, 2018, 16:157-168] PubMed: 29502045
Nitric oxide generation by the organic nitrate NDBP attenuates oxidative stress and angiotensin II-mediated hypertension [Porpino SK, et al. Br J Pharmacol, 2016, 173(14):2290-302] PubMed: 27160064
Inorganic nitrite attenuates NADPH oxidase-derived superoxide generation in activated macrophages via a nitric oxide-dependent mechanism. [Yang T, et al. Free Radic Biol Med, 2015, 10.1016/j.freeradbiomed.2015.02.016] PubMed: 25724690

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。