Home Immunology & Inflammation ROS inhibitor Febuxostat For research use only.

Febuxostat

Synonyms: TMX 67, TEI-6720

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

Febuxostat Chemical Structure

Febuxostat Chemical Structure

CAS: 144060-53-7

Selleck's Febuxostat has been cited by 6 Publications

2 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.98%
99.98

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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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05109936 Not yet recruiting
Gout
University Hospital Rouen
 January 1 2022 Phase 3
NCT04853160 Completed
Gout|Cardiovascular Diseases
Takeda
 August 15 2020 --
NCT04157959 Unknown status
Hyperuricemia
Jiangsu HengRui Medicine Co. Ltd.
 October 14 2019 Phase 1
NCT03918551 Completed
Bioequivalence
Pharmtechnology LLC|Altasciences Company Inc.
 May 3 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 316.37 Formula

C16H16N2O3S
CAS No. 144060-53-7 SDF Download Febuxostat SDF
Smiles CC1=C(SC(=N1)C2=CC(=C(C=C2)OCC(C)C)C#N)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 63 mg/mL ( (199.13 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 63 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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