CAS 144060-53-7|Febuxostat

Introduction：Basic information about CAS 144060-53-7|Febuxostat, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Febuxostat BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Customs
6. Synonyms

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	/	Flash Point	278.3±32.9 °C

Names

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

Febuxostat BiologicalActivity

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	Signaling Pathways >>Metabolic Enzyme/Protease >>Xanthine OxidaseResearch Areas >>Metabolic Disease
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.

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

Signaling Pathways >>Metabolic Enzyme/Protease >>Xanthine OxidaseResearch Areas >>Metabolic Disease

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
InChIKey	BQSJTQLCZDPROO-UHFFFAOYSA-N
SMILES	Cc1nc(-c2ccc(OCC(C)C)c(C#N)c2)sc1C(=O)O
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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