A potent inhibitor of xanthine oxidase; inhibits bovine milk xanthine oxidase as well as mouse and rat liver xanthine oxidase/xanthine dehydrogenase (IC50s = 1.4

Febuxostat – 5 mg

Brand:
Cayman
CAS:
144060-53-7
Storage:
-20
UN-No:
Non-Hazardous - /

Febuxostat is an antihyperuricemic nonpurine inhibitor of both the oxidized and reduced forms of xanthine oxidase.{22476} 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).{42215} It is 10-30 times more potent than the hypoxanthine analog allopurinol (Item No. 10012597; Kis = 0.7 nM and 0.7 μM, respectively).{22474,22475} Febuxostat decreases the serum level of urate in a potassium oxonate rat model of hyperuricemia (ED50 = 1.5 mg/kg).{42215} 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.{43642} 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).{42216} Formulations containing febuxostat have been used in the treatment of symptomatic hyperuricemia in patients with gout.  

 

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Description

A potent inhibitor of xanthine oxidase; 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); decreases serum urate levels in a potassium oxonate rat model of hyperuricemia (ED50 = 1.5 mg/kg); reduces hepatic macrovesicular steatosis in mice fed a high-fat diet containing trans fatty acids at 1 mg/kg per day; increases CNS expression of GOT2 and improves neurological symptoms in a mouse model of secondary progressive EAE

Formal name: 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methyl-5-thiazolecarboxylic acid

Synonyms:  FBX|TEI 6720|TMX 67

Molecular weight: 316.4

CAS: 144060-53-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Nucleic Acid Turnover/Signaling||Research Area|Endocrinology & Metabolism|Metabolic Diseases|NAFLD & NASH||Research Area|Neuroscience

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