Febuxostat

Modify Date: 2024-01-02 17:01:15

Febuxostat Structure
Febuxostat structure
 Common Name Febuxostat
CAS Number 144060-53-7 Molecular Weight 316.375
Density 1.3±0.1 g/cm3 Boiling Point 536.6±60.0 °C at 760 mmHg
Molecular Formula C16H16N2O3S Melting Point 238-239ºC
MSDS N/A Flash Point 278.3±32.9 °C

 Use of Febuxostat


Febuxostat(TEI 6720;TMX 67 ) is selective xanthine oxidase inhibitor with Ki of 0.6 nM.IC50 value: 0.6 nM (Ki) [1]Target: xanthine oxidasein 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 [1]. 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].

 Names

Name 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methyl-1,3-thiazole-5-carboxylic acid
Synonym More Synonyms

 Febuxostat Biological Activity

Description Febuxostat(TEI 6720;TMX 67 ) is selective xanthine oxidase inhibitor with Ki of 0.6 nM.IC50 value: 0.6 nM (Ki) [1]Target: xanthine oxidasein 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 [1]. 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].
Related Catalog
References

[1]. Takano Y, et al. Selectivity of febuxostat, a novel non-purine inhibitor of xanthine oxidase/xanthine dehydrogenase. Life Sci, 2005, 76(16), 1835-1847.

[2]. Sánchez-Lozada LG, et al. Effects of febuxostat on metabolic and renal alterations in rats with fructose-induced metabolic syndrome. Am J Physiol Renal Physiol, 2008, 294(4), F710-F718.

[3]. Sánchez-Lozada LG, et al. Effect of febuxostat on the progression of renal disease in 5/6 nephrectomy rats with and without hyperuricemia. Nephron Physiol, 2008, 108(4), p69-p78.

[4]. Xu X, et al. Xanthine oxidase inhibition with febuxostat attenuates systolic overload-induced left ventricular hypertrophy and dysfunction in mice. Card Fail, 2008, 14(9), 746-753.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 536.6±60.0 °C at 760 mmHg
Melting Point 238-239ºC
Molecular Formula C16H16N2O3S
Molecular Weight 316.375
Flash Point 278.3±32.9 °C
Exact Mass 316.088165
PSA 111.45000
LogP 4.87
Vapour Pressure 0.0±1.5 mmHg at 25°C
Index of Refraction 1.606
Storage condition Refrigerator

 Safety Information

Hazard Codes Xi
HS Code 2934100090

 Customs

HS Code 2934100090
Summary 2934100090 other compounds containing an unfused thiazole ring (whether or not hydrogenated) in the structure VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%

 Synonyms

2-(3-Cyano-4-(2-methylpropoxy)phenyl)-4-methylthiazole-5-carboxylic acid
Febuxostat
2-(3-Cyano-4-isobutoxyphenyl)-4-methylthiazole-5-carboxylic Acid,This product is unavailable
2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methyl-1,3-thiazole-5-carboxylic acid
5-Thiazolecarboxylic acid, 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methyl-
Uloric
5-Thiazolecarboxylic acid, 2-(3-cyano-4-(2-methylpropoxy)phenyl)-4-methyl-
Tei-6720
MFCD00871598
UNII-101V0R1N2E
Adenuric
Febuxostat,This product is unavailable
2-(3-Cyano-4-isobutoxyphenyl)-4-methyl-1,3-thiazole-5-carboxylic acid
TMX 67
2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid
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Febuxostat-d7
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Febuxostat sodium
1140907-13-6
Febuxostat Impurity 5
1239233-86-3
Febuxostat Impurity 1
1239233-87-4
Febuxostat impurity 8
144060-62-8
Febuxostat impurity 7
1350352-70-3
Febuxostat Impurity 2
1330632-46-6
Febuxostat impurity 6
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