Febuxostat

Catalog No.S1547 Batch:S154701

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Technical Data

Formula

C16H16N2O3S
Molecular Weight 316.37 CAS No. 144060-53-7
Solubility (25°C)* In vitro DMSO 63 mg/mL (199.13 mM)
Ethanol 63 mg/mL (199.13 mM)
Water 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Febuxostat (TMX 67, TEI-6720) is a selective xanthine oxidase inhibitor with Ki of 0.6 nM.
Targets
xanthine oxidase [1]
0.6 nM(Ki)
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]

Protocol (from reference)

Customer Product Validation

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

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

Selleck's Febuxostat has been cited by 6 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.