product name Febuxostat
Description: Febuxostat (also called TMX 67, TEI-6720) is a selective xanthine oxidase inhibitor with Ki of 0.6 nM. Febuxostat displayed potent mixed-type inhibition of the activity of xanthine oxidase (XO). Febuxostat was also reported to be 1000-fold (IC50=1.8 nM) more potent than allopurinol (IC50= 2.9 μM) at inhibiting XO-dependent uric acid formation. 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.
References: Life 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.
316.37
Formula
C16H16N2O3S
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)
Synonyms
TMX 67, TEI-6720
other peoduct :
| 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. Kinase Assay: 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 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. 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. |
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| References | Life 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. |
