Febuxostat-d9 Chemical Properties

Melting point:

>201°C (dec.)

storage temp. 

Refrigerator

solubility 

Chloroform (Slightly), Methanol (Slightly)

form 

Solid

color 

White to Off-White

Febuxostat-d9 Usage And Synthesis

Description

Febuxostat-d₉ is intended for use as an internal standard for the quantification of febuxostat by GC- or LC-MS. Febuxostat is an antihyperuricemic nonpurine inhibitor of both the oxidized and reduced forms of xanthine oxidase. It inhibits bovine milk xanthine oxidase as well as mouse and rat liver xanthine oxidase/xanthine dehydrogenase (IC₅₀s = 1.4, 1.8, and 2.2 nM, respectively). It is 10-30 times more potent than the hypoxanthine analog allopurinol (; K_is = 0.7 nM and 0.7 μM, respectively). Febuxostat decreases the serum level of urate in a potassium oxonate rat model of hyperuricemia (ED₅₀ = 1.5 mg/kg). It reduces hepatic macrovesicular steatosis in mice fed a high-fat diet containing trans fatty acids when administered at a dose of 1 mg/kg per day. Febuxostat (0.75 mg/kg) also increases CNS expression of glutamate oxaloacetate transaminase 2 (GOT2) and improves neurological symptoms in a mouse model of secondary progressive experimental autoimmune encephalomyelitis (EAE). Formulations containing febuxostat have been used in the treatment of symptomatic hyperuricemia in patients with gout.

Uses

Febuxostat-d9 is a Labeled compound, intended for use as an internal standard for the quantification of Febuxostat by GC- or LC-mass spectrometry.

Uses

Labelled Febuxostat (F229000). Xanthine oxidase/xanthine dehydrogenase inhibitor. Used for treatment of hyperuricemia and chronic gout.

References

[1] KEN OKAMOTO. An extremely potent inhibitor of xanthine oxidoreductase. Crystal structure of the enzyme-inhibitor complex and mechanism of inhibition.[J]. The Journal of Biological Chemistry, 2003, 278 3: 1848-1855. DOI: 10.1074/jbc.m208307200
[2] YOSHIO OSADA. Hypouricemic effect of the novel xanthine oxidase inhibitor, TEI-6720, in rodents[J]. European journal of pharmacology, 1993, 241 2: Pages 183-188. DOI: 10.1016/0014-2999(93)90201-r
[3] YASUHIRO TAKANO . Selectivity of febuxostat, a novel non-purine inhibitor of xanthine oxidase/xanthine dehydrogenase[J]. Life sciences, 2005, 76 16: Pages 1835-1847. DOI: 10.1016/j.lfs.2004.10.031
[4] MANISHA BISHT  S S B. Febuxostat: a novel agent for management of hyperuricemia in gout.[J]. Indian Journal of Pharmaceutical Sciences, 2011, 73 6: 597-600. DOI: 10.4103/0250-474x.100231
[5] YUSUKE NAKATSU. The xanthine oxidase inhibitor febuxostat suppresses development of nonalcoholic steatohepatitis in a rodent model.[J]. American journal of physiology. Gastrointestinal and liver physiology, 2015: G42-51. DOI: 10.1152/ajpgi.00443.2014
[6] JOSEPHE A HONORAT. Febuxostat ameliorates secondary progressive experimental autoimmune encephalomyelitis by restoring mitochondrial energy production in a GOT2-dependent manner.[J]. PLoS ONE, 2017: e0187215. DOI: 10.1371/journal.pone.0187215

Febuxostat-d9(1246819-50-0)Related Product Information

• Febuxostat
• 2-HYDROXY-THIOBENZAMIDE
• 2-[3-Carboxy-4-(2-Methylpropoxy)phenyl]-4-Methyl-5-thiazolecarboxylic Acid
• 2-[3-(AMinocarbonyl)-4-(2-Methylpropoxy)phenyl]-4-Methyl-5-thiazolecarboxylic Acid
• Ethyl 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylate
• Febuxostat impurity 37
• FeBuxostat Impurity 33
• 3-Cyano-4-isobutoxybenzoic acid
• ethyl 2-(3-formyl-4-hydroxyphenyl)-4-methyl thiazole-5-carboxylate
• ETHYL 2-(3-FORMYL-4-ISOBUTOXYPHENYL)-4-METHYLTHIAZOLE-5-CARBOXYLATE
• 4-ISOBUTOXY-BENZALDEHYDE
• 2-(3-cyano-4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid
• Febuxostat Impurity 6
• 3-Cyano-4-(2-methylpropoxy)benzenecarbothioamide
• isopropyl 2-(3-cyano-4-isobutoxyphenyl)-4-methylthiazole-5-carboxylate
• Febuxostat Impurity 8
• Febuxostat Impurity 14
• Febuxostat Bromo Impurity