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Febuxostat (TEI-6720) Xanthine Oxidase Inhibitor

Cat.No.S1547

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

Batch: Purity: 99.98%
99.98

Solubility

In vitro
Batch:

DMSO : 63 mg/mL (199.13 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous 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.

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Chemical Information, Storage & Stability

Molecular Weight 316.37 Formula

C16H16N2O3S

Storage (From the date of receipt)
CAS No. 144060-53-7 Download SDF Storage of Stock Solutions

Synonyms TMX 67, TEI-6720 SMILES CC1=C(SC(=N1)C2=CC(=C(C=C2)OCC(C)C)C#N)C(=O)O

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Mechanism of Action

Targets/IC50/Ki
xanthine oxidase
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.
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. This compound (5–6 mg/kg/day) combined with fructose also reduces glomerular pressure, renal vasoconstriction, and afferent arteriolar area in rats compared with fructose alone. It 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. This chemical (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. It 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. This agent 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. It 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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/18995179/
  • [5] https://pubmed.ncbi.nlm.nih.gov/22995295/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-01-08)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07326839 NOT_YET_RECRUITING
Gout; Obesity
XueMei Guo
2025-12-10
NCT07323095 NOT_YET_RECRUITING
Chronic Kidney Disease
Atom Therapeutics Co., Ltd
2026-06-30 PHASE2
NCT06834230 RECRUITING
Hyperuricemia or Gout; Hypertension
Saga University
2025-03-28 PHASE4
NCT07362355 RECRUITING
Primary Gout and Hyperuricemia
Jiangsu HengRui Medicine Co., Ltd.
2026-02-09 PHASE2
NCT07369622 NOT_YET_RECRUITING
Gout Initiating Urate-loweringUrate-lowering Therapy; Gout Arthritis; Gout and Hyperuricemia
Haiphong University of Medicine and Pharmacy
2026-01-20 PHASE4
NCT07485452 RECRUITING
Non-Small Cell Lung Cancer
Maastricht University Medical Center
2026-06 PHASE2

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