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Febuxostat(TEI 6720 TMX 67)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Febuxostat(TEI 6720 TMX 67)图片
CAS NO:144060-53-7
规格:≥98%
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议
1g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)316.37
FormulaC16H16N2O3S
CAS No.144060-53-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 63 mg/mL (199.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)Chemical Name: 2-(3-cyano-4-isobutoxyphenyl)-4-methylthiazole-5-carboxylic acid
InChi Key: BQSJTQLCZDPROO-UHFFFAOYSA-N
InChi Code: InChI=1S/C16H16N2O3S/c1-9(2)8-21-13-5-4-11(6-12(13)7-17)15-18-10(3)14(22-15)16(19)20/h4-6,9H,8H2,1-3H3,(H,19,20)
SMILES Code: O=C(C1=C(C)N=C(C2=CC=C(OCC(C)C)C(C#N)=C2)S1)O
SynonymsTMX 67, TEI-6720; TMX-67; TEI-6720; TEI 6720; TMX67; TEI6720; Uloric; Adenuric
实验参考方法
In Vitro

In vitro activity: 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.


Cell Assay: In a previous study, the authors investigated the effects of febuxostat on several enzymes in purine and pyrimidine metabolism and characterized the mechanism of febuxostat inhibition of XO activity. Results showed that Febuxostat displayed potent mixed-type inhibition of the activity of purified bovine milk XO, indicating inhibition of both the oxidized and reduced forms of XO.

In VivoFebuxostat (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. 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. 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. 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.
Animal model Rats
Formulation & Dosage 5–6 mg/kg/day
ReferencesLife Sci. 2005 Mar 4;76(16):1835-47. Epub 2005 Jan 18; Am J Physiol Renal Physiol. 2008 Apr;294(4):F710-8; Nephron Physiol. 2008;108(4):p69-78.