Febuxostat , ≥98% , 144060-53-7

Synonym(s):
2-(3-Cyano-4-isobutoxyphenyl)-4-methyl-1,3-thiazole-5-carboxylic acid;Adenuric;Atenuri;Uloric

CAS NO.：144060-53-7

Empirical Formula: C16H16N2O3S

Molecular Weight: 316.37

MDL number: MFCD00871598

EINECS: 682-158-6

PRODUCT Properties

• Melting point: 238-239°(dec.)
• Boiling point: 536.6±60.0 °C(Predicted)
• Density: 1.31±0.1 g/cm3(Predicted)
• storage temp.: 2-8°C
• solubility: DMSO (Slightly), Methanol (Slightly)
• pka: 2.48±0.10(Predicted)
• form: powder
• color: White to Off-White
• Merck: 14,3948
• InChI: InChI=1S/C16H16N2O3S/c1-9(2)8-21-13-5-4-11(6-12(13)7-17)15-18-10(3)14(22-15)16(19)20/h4-6,9H,8H2,1-3H3,(H,19,20)
• InChIKey: BQSJTQLCZDPROO-UHFFFAOYSA-N
• SMILES: S1C(C(O)=O)=C(C)N=C1C1=CC=C(OCC(C)C)C(C#N)=C1

Description and Uses

Febuxostat, a selective xanthine oxidase inhibitor, was launched for the chronic management of hyperuricemia in patients with gout. Hyperuricemia is defined as a serum uric acid concentration exceeding the limit of solubility. It predisposes affected persons to gout, a disease characterized by the formation of crystals of monosodium urate or uric acid from supersaturated fluids in joints and other tissues. Crystal deposition is asymptomatic, but it is revealed by bouts of joint inflammation. If left untreated, further crystals accumulate in joints and can form deposits known as tophi. A major aim in gout management is the long-term reduction of serum uric acid concentrations below saturation levels, as this results in crystal dissolution and eventual disappearance.
Febuxostat is a nonpurine derivative with higher potency and selectivity than allopurinol for inhibiting xanthine oxidase. It completely inhibits human xanthine oxidase activity in the lung cancer cell line A549, whereas the activities of other enzymes involved in purine or pyrimidine metabolism (e.g., purine nucleoside phosphorylase, adenosine deaminase, and pyrimidine nucleoside phosphorylase) are affected by<4%.

Febuxostat is a new generation xanthine oxidase inhibitor developed by Tejin Co. (Japan,) used clinically for for long-term treatment of hyperuicemia (gout,) a new and highly effective non-purine selective inhibitor of xanthine oxidase. 40-120 mg/day febuxostat was proven effective in lowering serum urate levels when administered to manage hyperuricemia in patients with gout. It is not recommended for gout patients without hyperuricemia.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302
• Precautionary statements: P264-P270-P301+P312-P330-P501
• RTECS: XJ3675310
• HS Code: 2934.10.2000