| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 5g |
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Purity: ≥98%
Febuxostat (formerly also called TMX 67, TEI-6720; TEI 6720; Uloric; TMX-67) is a potent and selective xanthine oxidase inhibitor with Ki of 0.6 nM and has been used to treat hyperuricemia and chronic gout. Febuxostat displayed potent mixed-type inhibition of the activity of xanthine oxidase (XO). Febuxostat was also reported to be 1000-fold (IC50=1.8 nM) more potent than allopurinol (IC50= 2.9 μM) at inhibiting XO-dependent uric acid formation. In a previous study, the authors investigated the effects of febuxostat on several enzymes in purine and pyrimidine metabolism and characterized the mechanism of febuxostat inhibition of XO activity. Results showed that Febuxostat displayed potent mixed-type inhibition of the activity of purified bovine milk XO, indicating inhibition of both the oxidized and reduced forms of XO.
| ln Vitro |
With Ki and Ki' values of 0.6 nM and 3.1 nM, respectively, showing inhibition of both the oxidized and reduced forms of xanthine oxidase, Febuxostat exhibits strong mixed-type suppression of the activity of pure bovine milk xanthine oxidase[1].
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| ln Vivo |
In comparison to fructose+P rats, rats given a high-fructose diet (i.e., 60% fructose) for 8 weeks showed significant reductions in lomerular pressure, renal vasoconstriction, and afferent arteriolar area when given febuxostat (5–6 mg/kg; i.e., daily for 4 weeks). However, rats given a normal diet showed no significant effects from febuxostat treatment alone[2]. In 5/6 Nx (5/6 nephrectomy) rats with and without concurrent hyperuricemia, febuxostat (3–4 mg/kg; po; daily for 4 weeks) combined with oxonic acid (750 mg/kg; oral gavage; daily for 4 weeks) prevents renal injury[3]. Febuxostat (2.5 mg/kg; po; daily for 12 weeks) lowers the amount of ROS in the aorta wall of atherosclerotic animals and prevents the formation of plaque in ApoE−/− mice[4]. The antidepressant effect of fruxostat (15.6 mg/kg; po; once daily for 21 days) is demonstrated by a substantial reduction in the immobility time in the forced swimming test (FST) in mice [5]. When administered in conjunction with doxorubicin (10 mg/kg; po; daily for 21 days), fruxostat (10 mg/kg; po; po; daily for 21 days) significantly reduced nephrotoxicity indicators and inflammatory mediators, restored oxidative stress biomarker levels to normal, and inhibited the expression of renal caspase-3[6].
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| References |
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| Additional Infomation |
Pharmacodynamics
Febuxostat is a novel, selective xanthine oxidase/dehydrogenase inhibitor that works by decreasing serum uric acid in a dose-dependent manner. In healthy subjects, febuxostat decreased the mean serum uric acid and serum xanthine concentrations, as well as the total urinary uric acid excretion. Febuxostat at daily doses of 40-80 mg reduced the 24-hour mean serum uric acid concentrations by 40 to 55%. Closely related to the drug-induced reduction of serum uric acid levels and mobilization of urate crystals in tissue deposits, febuxostat is associated with gout flares. Unlike [allopurinol] and [oxypurinol], febuxostat has no inhibitory actions against other enzymes involved in purine and pyrimidine synthesis and metabolism, because it does not structurally resemble purines or pyrimidines. |
| Molecular Formula |
C16H16N2O3S
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| Molecular Weight |
316.37
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| Exact Mass |
316.088
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| CAS # |
144060-53-7
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| Related CAS # |
Febuxostat-d9;1246819-50-0;Febuxostat sodium;1140907-13-6;Febuxostat-d7;1285539-74-3
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
536.6±60.0 °C at 760 mmHg
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| Melting Point |
238-239ºC
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| Flash Point |
278.3±32.9 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.606
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| LogP |
4.87
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| InChi Key |
BQSJTQLCZDPROO-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methyl-1,3-thiazole-5-carboxylic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1609 mL | 15.8043 mL | 31.6086 mL | |
| 5 mM | 0.6322 mL | 3.1609 mL | 6.3217 mL | |
| 10 mM | 0.3161 mL | 1.5804 mL | 3.1609 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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