Febuxostat Inhibitor CAS No. 144060-53-7

Cat. No.	Name	Size	Price
KI0870	Febuxostat	10 mg	$176
	Febuxostat	25 mg	$336
	Febuxostat	50 mg	$592
	Febuxostat	100 mg	$1072

Chemical Characteristic

Product Name	Febuxostat
Synonyms	TEI-6720, TMX-67, Uloric
CAS No.	144060-53-7
Molecular Weight	316.37
Formula	C₁₆H₁₆N₂O₃S
Chemical Structure

Biological activities

Febuxostat is a potent non-purine inhibitor of xanthine oxidase (XO). Febuxostat is used for the treatment of hyperuricemia and gout. Febuxostat is a potent, mixed-type inhibitor of bovine milk XO.^[1] Febuxostat has a weak inhibitory effect on CYP2D6 with a Ki of 40 µM. ^[2] The IC50 of febuxostat for bovine milk XO is 20 nM. ^[3] Febuxostat potently inhibits XO-dependent uric acid formation with an IC50 of 1.8 nM. Febuxostat also inhibits GAG-immobilized XO with an IC50 of 4.4 nM. ^[4] Febuxostat has a potent in vivo hypouricemic effect in rodents and chimpanzees. ^[1] Febuxostat lowers serum urate (sUA) levels more potently than allopurinol. ^[5] Febuxostat can bind to albumin in vivo. ^[6]

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. 閵嗏偓閵嗏偓 [2] R.?Khosravan?PhD, et al. Effect of febuxostat on pharmacokinetics of desipramine, a CYP2D6 substrate, in healthy subjects. Clinical Pharmacology & Therapeutics. 2005, 77: 43. 閵嗏偓閵嗏偓 [3] Edwards NL, et al. Febuxostat: a new treatment for hyperuricaemia in gout. Rheumatology (Oxford). 2009, 48 Suppl 2: ii15-ii19. 閵嗏偓閵嗏偓 [4] Malik UZ, et al. Febuxostat inhibition of endothelial-bound XO: implications for targeting vascular ROS production. Free Radic Biol Med. 2011, 51(1): 179-184. 閵嗏偓閵嗏偓 [5] Komoriya K, et al. Pharmacokinetics and pharmacodynamics of febuxostat (TMX-67), a non-purine selective inhibitor of xanthine oxidase/xanthine dehydrogenase (NPSIXO) in patients with gout and/or hyperuricemia. Nucleosides Nucleotides Nucleic Acids. 2004, 23(8-9): 1119-1122. 閵嗏偓閵嗏偓 [6] Mukoyoshi M, et al. In vitro drug-drug interaction studies with febuxostat, a novel non-purine selective inhibitor of xanthine oxidase: plasma protein binding, identification of metabolic enzymes and cytochrome P450 inhibition. Xenobiotica. 2008, 38(5): 496-510. 閵嗏偓閵嗏偓

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