Febuxostat

Catalog No.S1547 Synonyms: TMX 67, TEI-6720

Febuxostat Chemical Structure

Molecular Weight(MW): 316.37

Febuxostat is a selective xanthine oxidase inhibitor with Ki of 0.6 nM.

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2 Customer Reviews

  • NOX activity was measured as lucigenin-dependent chemiluminescence of superoxide. Incubation with febuxostat increased superoxide generation in nonactivated macrophages, but did not significantly influence superoxide formation in LPS-activated macrophages. Simultaneous treatment with febuxostat abolished the effect of nitrite during activation with LPS. Data are means±SEM (n=10-12). *, p<0.05.  LPS, lipopolysaccharide (10 ng/ml); NO2, sodium nitrite (10 μM); febuxostat, xanthine oxidase inhibitor (30 nM).

    Free Radical Biology and Medicine, 2015, 159-166.. Febuxostat purchased from Selleck.

    Effect of NDBP on NOX activity in liver (A) homogenates. (A) Dose-dependent response to NDBP in liver and during simultaneous inhibition of xanthine oxidase with febuxostat (Feb; 30 nM) (n = 5 per group). *P < 0.05.

    Br J Pharmacol, 2016, 173(14):2290-302.. Febuxostat purchased from Selleck.

Purity & Quality Control

Choose Selective ROS Inhibitors

Biological Activity

Description Febuxostat 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

Solubility (25°C)

In vitro DMSO 63 mg/mL (199.13 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 316.37
Formula

C16H16N2O3S

CAS No. 144060-53-7
Storage powder
Synonyms TMX 67, TEI-6720

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02579096 Not yet recruiting Gout|Chronic Kidney Diseases VA Office of Research and Development November 2016 Phase 4
NCT02944214 Not yet recruiting Chronic Kidney Disease|Hyperuricemia|Abnormal Renal Function Shanghai 10th Peoples Hospital October 2016 --
NCT02866214 Completed Endothelial Dysfunction|Endstage Renal Disease Ain Shams University August 2016 Phase 2|Phase 3
NCT02504320 Completed Healthy Volunteers Takeda August 2015 Phase 1
NCT02500641 Active, not recruiting Gout Menarini International Operations Luxembourg SA July 2015 Phase 4
NCT02382640 Completed Healthy Volunteers Takeda March 2015 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID