MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 328907 | Name: Febuxostat
Featured

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Febuxostat, also known as Uloric and TMX-67, is a xanthine oxidase inhibitor used to treat hyperuricemia and chronic gout.

Chemical Structure

Febuxostat
Febuxostat
CAS#144060-53-7 (free acid)

Theoretical Analysis

MedKoo Cat#: 328907

Name: Febuxostat

CAS#: 144060-53-7 (free acid)

Chemical Formula: C16H16N2O3S

Exact Mass: 316.0882

Molecular Weight: 316.38

Elemental Analysis: C, 60.74; H, 5.10; N, 8.85; O, 15.17; S, 10.13

Price and Availability

Size Price Availability Quantity
1g USD 250.00 2 Weeks
2g USD 400.00 2 Weeks
5g USD 650.00 2 Weeks
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
144060-53-7 (free acid) 442664-09-7 (hemihydrate)
Synonym
Febuxostat; Uloric; Adenuric; FBX; TMX-67; TMX 67; TMX67; TEI6720; TEI 6720; TEI-6720; NSC-758874; NSC 758874; NSC758874
IUPAC/Chemical Name
2-(3-cyano-4-isobutoxyphenyl)-4-methylthiazole-5-carboxylic acid
InChi Key
BQSJTQLCZDPROO-UHFFFAOYSA-N
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)
SMILES Code
O=C(C1=C(C)N=C(C2=CC=C(OCC(C)C)C(C#N)=C2)S1)O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Febuxostat (TEI 6720) is selective xanthine oxidase inhibitor with a Ki of 0.6 nM.
In vitro activity:
The gene expression level of iNOS was significantly increased by stimulation with IL-18 but greatly suppressed by the introduction of Febuxostat (Figure 4A). The increased release of NO induced by stimulation with IL-18 was significantly inhibited in the presence of Febuxostat (Figure 4B). Reference: Am J Transl Res. 2021; 13(3): 979–987. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8014396/
In vivo activity:
The gingival expression of TNF-α, IL-1β, 4-HNE, and 8-OHdG was up-regulated in rats with periodontitis. Febuxostat significantly reduced alveolar bone loss, proinflammatory cytokine levels, and oxidative stress. Reference: Pharmacology. 2021;106(5-6):294-304. https://pubmed.ncbi.nlm.nih.gov/33735887/
Solvent mg/mL mM
Solubility
DMSO 36.7 115.94
DMF 30.0 94.82
DMF:PBS (pH 7.2) (1:1) 0.5 1.58
Ethanol 10.4 32.90
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 316.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Geng Q, Zhang H, Cui Y, Wei Q, Wang S. Febuxostat mitigates IL-18-induced inflammatory response and reduction of extracellular matrix gene. Am J Transl Res. 2021 Mar 15;13(3):979-987. PMID: 33841634; PMCID: PMC8014396. 2. Hao J, Zhang W, Tong R, Huang Z. Febuxostat Prevents the Cytotoxicity of Propofol in Brain Endothelial Cells. ACS Omega. 2021 Feb 15;6(8):5471-5478. doi: 10.1021/acsomega.0c05708. PMID: 33681587; PMCID: PMC7931401. 3. Tsukamoto T, Tsujii M, Odake K, Iino T, Nakamura T, Matsumine A, Sudo A. Febuxostat reduces muscle wasting in tumor-bearing mice with LM8 osteosarcoma cells via inhibition of reactive oxygen species generation. Free Radic Res. 2021 Jul 19:1-11. doi: 10.1080/10715762.2021.1947502. Epub ahead of print. PMID: 34278932. 4. Nessa N, Kobara M, Toba H, Adachi T, Yamamoto T, Kanamura N, Pezzotti G, Nakata T. Febuxostat Attenuates the Progression of Periodontitis in Rats. Pharmacology. 2021;106(5-6):294-304. doi: 10.1159/000513034. Epub 2021 Mar 18. PMID: 33735887.
In vitro protocol:
1. Geng Q, Zhang H, Cui Y, Wei Q, Wang S. Febuxostat mitigates IL-18-induced inflammatory response and reduction of extracellular matrix gene. Am J Transl Res. 2021 Mar 15;13(3):979-987. PMID: 33841634; PMCID: PMC8014396. 2. Hao J, Zhang W, Tong R, Huang Z. Febuxostat Prevents the Cytotoxicity of Propofol in Brain Endothelial Cells. ACS Omega. 2021 Feb 15;6(8):5471-5478. doi: 10.1021/acsomega.0c05708. PMID: 33681587; PMCID: PMC7931401.
In vivo protocol:
1. Tsukamoto T, Tsujii M, Odake K, Iino T, Nakamura T, Matsumine A, Sudo A. Febuxostat reduces muscle wasting in tumor-bearing mice with LM8 osteosarcoma cells via inhibition of reactive oxygen species generation. Free Radic Res. 2021 Jul 19:1-11. doi: 10.1080/10715762.2021.1947502. Epub ahead of print. PMID: 34278932. 2. Nessa N, Kobara M, Toba H, Adachi T, Yamamoto T, Kanamura N, Pezzotti G, Nakata T. Febuxostat Attenuates the Progression of Periodontitis in Rats. Pharmacology. 2021;106(5-6):294-304. doi: 10.1159/000513034. Epub 2021 Mar 18. PMID: 33735887.
1: Sircar D, Chatterjee S, Waikhom R, Golay V, Raychaudhury A, Chatterjee S, Pandey R. Efficacy of Febuxostat for Slowing the GFR Decline in Patients With CKD and Asymptomatic Hyperuricemia: A 6-Month, Double-Blind, Randomized, Placebo-Controlled Trial. Am J Kidney Dis. 2015 Dec;66(6):945-50. doi: 10.1053/j.ajkd.2015.05.017. Epub 2015 Jul 30. PubMed PMID: 26233732. 2: Tanaka K, Nakayama M, Kanno M, Kimura H, Watanabe K, Tani Y, Hayashi Y, Asahi K, Terawaki H, Watanabe T. Renoprotective effects of febuxostat in hyperuricemic patients with chronic kidney disease: a parallel-group, randomized, controlled trial. Clin Exp Nephrol. 2015 Dec;19(6):1044-53. doi: 10.1007/s10157-015-1095-1. Epub 2015 Feb 13. PubMed PMID: 25676011. 3: Zhou H, Zheng Y, Wu G, Hu X, Zhai Y, Iv D, Liu J, Wu L, Shentu J. Pharmacokinetics and tolerability of febuxostat after oral administration in healthy Chinese volunteers: a randomized, open-label, singleand multiple-dose three-way crossover study. Int J Clin Pharmacol Ther. 2016 Feb;54(2):115-24. doi: 10.5414/CP202394. PubMed PMID: 26636422. 4: Tsuruta Y, Kikuchi K, Tsuruta Y, Sasaki Y, Moriyama T, Itabashi M, Takei T, Uchida K, Akiba T, Tsuchiya K, Nitta K. Febuxostat improves endothelial function in hemodialysis patients with hyperuricemia: A randomized controlled study. Hemodial Int. 2015 Oct;19(4):514-20. doi: 10.1111/hdi.12313. Epub 2015 May 21. PubMed PMID: 25998500. 5: Luo Z, Nan F, Miao J, Chen Z, Li M, Liang M. Pharmacokinetics and Bioequivalence of Two Formulations of Febuxostat 40-Mg and 80-Mg Tablets: A Randomized, Open-Label, 4-Way Crossover Study in Healthy Chinese Male Volunteers. PLoS One. 2016 Mar 14;11(3):e0150661. doi: 10.1371/journal.pone.0150661. eCollection 2016. PubMed PMID: 26974539; PubMed Central PMCID: PMC4790952. 6: Tani S, Nagao K, Hirayama A. Effect of Febuxostat, a Xanthine Oxidase Inhibitor, on Cardiovascular Risk in Hyperuricemic Patients with Hypertension: A Prospective, Open-label, Pilot Study. Clin Drug Investig. 2015 Dec;35(12):823-31. doi: 10.1007/s40261-015-0349-8. PubMed PMID: 26482071. 7: Spina M, Nagy Z, Ribera JM, Federico M, Aurer I, Jordan K, Borsaru G, Pristupa AS, Bosi A, Grosicki S, Glushko NL, Ristic D, Jakucs J, Montesinos P, Mayer J, Rego EM, Baldini S, Scartoni S, Capriati A, Maggi CA, Simonelli C; FLORENCE Study Group. FLORENCE: a randomized, double-blind, phase III pivotal study of febuxostat versus allopurinol for the prevention of tumor lysis syndrome (TLS) in patients with hematologic malignancies at intermediate to high TLS risk. Ann Oncol. 2015 Oct;26(10):2155-61. doi: 10.1093/annonc/mdv317. Epub 2015 Jul 27. PubMed PMID: 26216382. 8: Wu Y, Mao Z, Liu Y, Wang X, Di X. Simultaneous determination of febuxostat and its three active metabolites in human plasma by liquid chromatography-tandem mass spectrometry and its application to a pharmacokinetic study in Chinese healthy volunteers. J Pharm Biomed Anal. 2015 Oct 10;114:216-21. doi: 10.1016/j.jpba.2015.05.020. Epub 2015 Jun 11. PubMed PMID: 26072013. 9: Sezai A, Soma M, Nakata K, Osaka S, Ishii Y, Yaoita H, Hata H, Shiono M. Comparison of febuxostat and allopurinol for hyperuricemia in cardiac surgery patients with chronic kidney disease (NU-FLASH trial for CKD). J Cardiol. 2015 Oct;66(4):298-303. doi: 10.1016/j.jjcc.2014.12.017. Epub 2015 Jan 31. PubMed PMID: 25649025. 10: Altan A, Shiozawa A, Bancroft T, Singh JA. A Real-World Study of Switching From Allopurinol to Febuxostat in a Health Plan Database. J Clin Rheumatol. 2015 Dec;21(8):411-8. doi: 10.1097/RHU.0000000000000322. PubMed PMID: 26580304; PubMed Central PMCID: PMC4654265. 11: Yamamoto T, Hidaka Y, Inaba M, Ishimura E, Ooyama H, Kakuta H, Moriwaki Y, Higami K, Ohtawara A, Hosoya T, Nishikawa H, Taniguchi A, Ueda T, Yamauchi T, Fujimori S, Mineo I, Yamanaka H. Effects of febuxostat on serum urate level in Japanese hyperuricemia patients. Mod Rheumatol. 2015 Sep;25(5):779-83. doi: 10.3109/14397595.2015.1016257. Epub 2015 Jun 12. PubMed PMID: 25671406. 12: Nishizawa T, Taniura T, Nomura S. Effects of febuxostat on platelet-derived microparticles and adiponectin in patients with hyperuricemia. Blood Coagul Fibrinolysis. 2015 Dec;26(8):887-92. doi: 10.1097/MBC.0000000000000335. PubMed PMID: 26164850; PubMed Central PMCID: PMC4664023. 13: Xu S, Liu X, Ming J, Chen S, Wang Y, Liu X, Liu H, Peng Y, Wang J, Lin J, Ji H, Liu B, Lu Y, Liu P, Zhang Y, Ji Q. A phase 3, multicenter, randomized, allopurinol-controlled study assessing the safety and efficacy of oral febuxostat in Chinese gout patients with hyperuricemia. Int J Rheum Dis. 2015 Jul;18(6):669-78. doi: 10.1111/1756-185X.12648. Epub 2015 May 27. PubMed PMID: 26013187. 14: Fukui T, Maruyama M, Yamauchi K, Yoshitaka S, Yasuda T, Abe Y. Effects of Febuxostat on Oxidative Stress. Clin Ther. 2015 Jul 1;37(7):1396-401. doi: 10.1016/j.clinthera.2015.03.026. Epub 2015 Apr 23. PubMed PMID: 25913922. 15: Wang S, Li Y, Song X, Wang X, Zhao C, Chen A, Yang P. Febuxostat pretreatment attenuates myocardial ischemia/reperfusion injury via mitochondrial apoptosis. J Transl Med. 2015 Jul 2;13:209. doi: 10.1186/s12967-015-0578-x. PubMed PMID: 26136232; PubMed Central PMCID: PMC4489215.

View History

Yadanzioside C

Yadanzioside C