Febuxostat - CAS 144060-53-7
Catalog number: 144060-53-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C16H16N2O3S
Molecular Weight:
316.37
COA:
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Targets:
IDO | Xanthine oxidase (XAO)
Description:
A potent IDO inhibitor
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Brife Description:
A potent IDO inhibitor
Purity:
> 98%
Appearance:
Solid powder
Synonyms:
TEI 6720; TMX 67; 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methyl-1,3-thiazole-5-carboxylic acid
Solubility:
Soluble to 75 mM in DMSO and to 50 mM in ethanol
Storage:
Store at RT
MSDS:
Inquire
Quality Standard:
In-house
Quantity:
Grams-Kilos
Melting Point:
238-239°(dec.)
InChIKey:
BQSJTQLCZDPROO-UHFFFAOYSA-N
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)
Canonical SMILES:
CC1=C(SC(=N1)C2=CC(=C(C=C2)OCC(C)C)C#N)C(=O)O
1.Determination of Febuxostat in Human Plasma Using RP-LC-UV Method.
Younes KM1, El-Kady EF2, Elzanfaly ES3. J Chromatogr Sci. 2016 Apr 11. pii: bmw040. [Epub ahead of print]
A simple and sensitive bioanalytical high-performance liquid chromatographic method with ultraviolet detection was developed and validated for the quantification of febuxostat (FEB) in human plasma. Ketoprofen was used as an internal standard. The analytes were extracted from human plasma samples by precipitation with acetonitrile. The reconstituted samples were chromatographed on C18 Bondapack 10 µm, 250 × 4.6 mm, Waters Column (Ireland) by using a mixture of acetonitrile and 0.5% aqueous phosphoric acid (pH 3) (52 : 48, v/v) as the mobile phase. The chromatographic separation was isocratically performed at room temperature at a flow rate of 1.0 mL/min with UV detection at 315 nm. The method exhibited a linear dynamic range over 0.05-5.00 µg/mL FEB in human plasma. The lower limit of quantification was 0.05 µg/mL. The results of the intra- and interday precision and accuracy studies were within the acceptable limits. The validated method was successfully applied for the determination of FEB in human plasma samples for application in bioequivalence studies.
2.Efficacy and safety of febuxostat for prevention of tumor lysis syndrome in patients with malignant tumors receiving chemotherapy: a phase III, randomized, multi-center trial comparing febuxostat and allopurinol.
Tamura K1, Kawai Y2, Kiguchi T3, Okamoto M4, Kaneko M5, Maemondo M6, Gemba K7, Fujimaki K8, Kirito K9, Goto T10, Fujisaki T11, Takeda K12, Nakajima A13, Ueda T14. Int J Clin Oncol. 2016 Mar 26. [Epub ahead of print]
BACKGROUND: Control of serum uric acid (sUA) levels is very important during chemotherapy in patients with malignant tumors, as the risks of tumor lysis syndrome (TLS) and renal events are increased with increasing levels of sUA. We investigated the efficacy and safety of febuxostat, a potent non-purine xanthine oxidase inhibitor, compared with allopurinol for prevention of hyperuricemia in patients with malignant tumors, including solid tumors, receiving chemotherapy in Japan.
3.Effects of topiroxostat and febuxostat on urinary albumin excretion and plasma xanthine oxidoreductase activity in db/db mice.
Nakamura T1, Murase T2, Nampei M3, Morimoto N3, Ashizawa N4, Iwanaga T4, Sakamoto R5. Eur J Pharmacol. 2016 Jun 5;780:224-31. doi: 10.1016/j.ejphar.2016.03.055. Epub 2016 Mar 30.
Topiroxostat, a xanthine oxidoreductase (XOR) inhibitor, has been shown to decrease the urinary albumin-to-creatinine ratio compared with placebo in hyperuricemic patients with stage 3 chronic kidney disease. Thus, we aimed to ascertain the albuminuria-lowering effect of topiroxostat in diabetic mouse. Db/db mice were fed standard diets with or without topiroxostat (0.1, 0.3, 1, and 3mg/kg/day) and febuxostat (0.1, 0.3, and 1mg/kg/day) for four weeks. Urinary albumin and purine bodies levels, XOR activities, and drug concentrations in the liver, kidney, and plasma were measured. Moreover, the XOR inhibitory activity of each XOR inhibitor was evaluated with or without an exogenous protein in vitro. Topiroxostat decreased dose-dependently the urinary albumin excretion, but febuxostat did not show such a tendency. Treatment with topiroxostat inhibited plasma XOR activity with dose-dependent increase in plasma purine levels, which was not observed by febuxostat.
4.Rationale, design, and baseline characteristics of a study to evaluate the effect of febuxostat in preventing cerebral, cardiovascular, and renal events in patients with hyperuricemia.
Kojima S1, Matsui K2, Ogawa H3, Jinnouchi H4, Hiramitsu S5, Hayashi T6, Yokota N7, Kawai N8, Tokutake E9, Uchiyama K10, Sugawara M11, Kakuda H12, Wakasa Y13, Mori H14, Hisatome I15, Waki M16, Ohya Y17, Kimura K18, Saito Y19; Febuxostat for Cerebral and Ca J Cardiol. 2016 Mar 18. pii: S0914-5087(16)00062-9. doi: 10.1016/j.jjcc.2016.02.015. [Epub ahead of print]
BACKGROUND: Since uric acid is associated with cardiovascular and renal disease, a treatment to maintain blood uric acid level may be required in patients with hyperuricemia. This study aims to evaluate preventive effects of febuxostat, a selective xanthine oxidase inhibitor, on cerebral, cardiovascular, and renal events in patients with hyperuricemia compared to conventional treatment.
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CAS 144060-53-7 Febuxostat

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