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Febuxostat

Name: Febuxostat
Brand: Selleck Chemicals
SKU: S1547
Rating: 5 (6 reviews)

Synonyms: TMX 67, TEI-6720

Catalog No.S1547 Purity: 99.98%

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

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 K_i 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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

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Chemical lnformation & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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