Febuxostat

SKU: orb1226272

Description

Febuxostat is a Xanthine Oxidase Inhibitor. The mechanism of action of febuxostat is as a Xanthine Oxidase Inhibitor. (In 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.(In Vivo):Febuxostat (5-6 mg/kg; i.e.; daily for 4 weeks) (fed a high-fructose diet (60% fructose) for 8 wk) significantly reduces lomerular pressure, renal vasoconstriction, and afferent arteriolar area relative to fructose+P rats, and shows no significant effects in rats on a normal diet when febuxostat treatment alone.Febuxostat (3-4 mg/kg; p.o.; daily for 4 weeks) with oxonic acid (750 mg/kg; oral gavage; daily for 4 weeks) preventes renal injury in 5/6 Nx (5/6 nephrectomy) rats with and without coexisting hyperuricemia.Febuxostat (2.5 mg/kg; p.o.; daily for 12 weeks) inhibits plaque formation in ApoE / mice and reduces the levels of ROS in the aortic wall of atherosclerotic mice.Febuxostat (15.6 mg/kg; p.o.; once daily for 21 successive days) shows antidepressant effect by significantly reduces the immobility time in the FST in mouse.Febuxostat (10 mg/kg; p.o.; daily for 21 days) administration with doxorubicin caused a significant decrease in nephrotoxicity markers and inflammatory mediators, restoration of normal values of oxidative stress biomarkers and hampering the expression of renal caspase-3.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 144060-53-7
• MW: 316.37
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₆N₂O₃S
• SMILES: O=C(C1=C(C)N=C(C2=CC=C(OCC(C)C)C(C#N)=C2)S1)O
• Target: ROS
• Solubility: DMSO: 63 mg/mL (199.13 mM)

Bioactivity

• In Vivo:
  Febuxostat (5-6 mg/kg; i. e. ; daily for 4 weeks) (fed a high-fructose diet (60% fructose) for 8 wk) significantly reduces lomerular pressure, renal vasoconstriction, and afferent arteriolar area relative to fructose+P rats, and shows no significant effects in rats on a normal diet when febuxostat treatment alone. Febuxostat (3-4 mg/kg; p.o. ; daily for 4 weeks) with oxonic acid (750 mg/kg; oral gavage; daily for 4 weeks) preventes renal injury in 5/6 Nx (5/6 nephrectomy) rats with and without coexisting hyperuricemia. Febuxostat (2.5 mg/kg; p.o. ; daily for 12 weeks) inhibits plaque formation in ApoE / mice and reduces the levels of ROS in the aortic wall of atherosclerotic mice. Febuxostat (15.6 mg/kg; p.o. ; once daily for 21 successive days) shows antidepressant effect by significantly reduces the immobility time in the FST in mouse. Febuxostat (10 mg/kg; p.o. ; daily for 21 days) administration with doxorubicin caused a significant decrease in nephrotoxicity markers and inflammatory mediators, restoration of normal values of oxidative stress biomarkers and hampering the expression of renal caspase-3.
  Read more...
• In 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.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

FBX | TEI 6720 | TMX 67

Quick Database Links

Gene Symbol

ROS