Febuxostat | Uloric | TMX-67 | CAS#144060-53-7 | Xanthine Oxidase Inhibitor

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

MedKoo CAT#: 328907

CAS#: 144060-53-7

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

Chemical Structure

Febuxostat

CAS# 144060-53-7

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 328907
Name: Febuxostat
CAS#: 144060-53-7
Chemical Formula: C16H16N2O3S
Exact Mass: 316.09
Molecular Weight: 316.375
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 220
2g	USD 400
5g	USD 650
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Febuxostat; TMX-67; TEI-6720; TMX 67; TEI 6720; TMX67; TEI6720; Uloric; Adenuric

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/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. 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

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.

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.

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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.

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