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MedKoo Cat#: 314261 | Name: Topiroxostat
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Description:

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

Topiroxostat (INN; trade names Topiloric, Uriadec) is a drug for the treatment of gout and hyperuricemia. It was approved for use in Japan in June 2013. Topiroxostat is a xanthine oxidase inhibitor which reduces serum urate levels.

Chemical Structure

Topiroxostat
CAS#577778-58-6

Theoretical Analysis

MedKoo Cat#: 314261

Name: Topiroxostat

CAS#: 577778-58-6

Chemical Formula: C13H8N6

Exact Mass: 248.0810

Molecular Weight: 248.24

Elemental Analysis: C, 62.90; H, 3.25; N, 33.85

Price and Availability

Size Price Availability Quantity
10mg USD 150.00
25mg USD 250.00
50mg USD 450.00
100mg USD 650.00
200mg USD 950.00
500mg USD 1,650.00
1g USD 2,250.00
2g USD 3,250.00
5g USD 4,250.00
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Related CAS #
No Data
Synonym
FYX051; FYX051; FYX 051; Topiroxostat. trade names Topiloric Uriadec.
IUPAC/Chemical Name
4-(5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl)picolinonitrile
InChi Key
UBVZQGOVTLIHLH-UHFFFAOYSA-N
InChi Code
InChI=1S/C13H8N6/c14-8-11-7-10(3-6-16-11)13-17-12(18-19-13)9-1-4-15-5-2-9/h1-7H,(H,17,18,19)
SMILES Code
N#CC1=NC=CC(C2=NNC(C3=CC=NC=C3)=N2)=C1
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

Preparing Stock Solutions

The following data is based on the product molecular weight 248.24 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
1: Zhong T, Huang K, Han L, Pang W, Xia Y, Qu S, Yu G, Chen Y, Fan H. Characterizing Pharmacokinetic Variability of Topiroxostat in Chinese Population: Insights from a Phase I Randomized Clinical Trial. Curr Drug Metab. 2024 Dec 16. doi: 10.2174/0113892002348045241210071452. Epub ahead of print. PMID: 39686641. 2: Chandrashekara S, Mahesh E. Topiroxostat-A Safer Uricostatic Drug with Enhanced Renal Protection: A Narrative Review. J Assoc Physicians India. 2024 Nov;72(11):73-79. doi: 10.59556/japi.72.0724. PMID: 39563126. 3: Chen WB, Hu GA, Dong BC, Sun HY, Lu DZ, Ru MY, Yu YL, Wang H, Wei B. Insights into the modulatory effects of host-gut microbial xanthine co-metabolism on high-fat diet-fed mice. Biochem Pharmacol. 2024 Dec;230(Pt 2):116596. doi: 10.1016/j.bcp.2024.116596. Epub 2024 Oct 29. PMID: 39481656. 4: Ishii T, Seya N, Taguri M, Wakui H, Yoshimura A, Tamura K. Allopurinol, Febuxostat, and Nonuse of Xanthine Oxidoreductase Inhibitor Treatment in Patients Receiving Hemodialysis: A Longitudinal Analysis. Kidney Med. 2024 Aug 28;6(11):100896. doi: 10.1016/j.xkme.2024.100896. PMID: 39347518; PMCID: PMC11437761. 5: Rana R, Sharma A, Kumar N, Khanna A, Jyoti, Dhir M, Gulati HK, Singh JV, Bedi PMS. A comprehensive review of synthetic and semisynthetic xanthine oxidase inhibitors: identification of potential leads based on in-silico computed ADME characteristics. Mol Divers. 2024 Aug 20. doi: 10.1007/s11030-024-10962-1. Epub ahead of print. PMID: 39164505. 6: Hagiwara M, Ishiyama S, Nakamura T, Mochizuki K. Topiroxostat improves glomerulosclerosis in type 2 diabetic Nagoya Shibata Yasuda mice with early diabetic kidney disease. Eur J Pharmacol. 2024 Nov 5;982:176915. doi: 10.1016/j.ejphar.2024.176915. Epub 2024 Aug 16. PMID: 39154822. 7: Sun Q, Yu W, Gong M, Ma J, Liu G, Mei T, Luo X. Xanthine oxidase immobilized cellulose membrane-based colorimetric biosensor for screening and detecting the bioactivity of xanthine oxidase inhibitors. Int J Biol Macromol. 2024 Aug;275(Pt 1):133450. doi: 10.1016/j.ijbiomac.2024.133450. Epub 2024 Jun 27. PMID: 38944077. 8: Liang JH, Yi XL, Gong JM, Du Z. Evaluation of the inhibitory effects of antigout drugs on human carboxylesterases in vitro. Toxicol In Vitro. 2024 Jun;98:105833. doi: 10.1016/j.tiv.2024.105833. Epub 2024 Apr 24. PMID: 38670244. 9: Yasir M, Park J, Han ET, Park WS, Han JH, Chun W. Drug Repositioning via Graph Neural Networks: Identifying Novel JAK2 Inhibitors from FDA-Approved Drugs through Molecular Docking and Biological Validation. Molecules. 2024 Mar 19;29(6):1363. doi: 10.3390/molecules29061363. PMID: 38542998; PMCID: PMC10974395. 10: Yamamoto T, Kasahara M, Ueshima K, Uemura S, Kashihara N, Kimura K, Konta T, Shoji T, Mima A, Mukoyama M, Saito Y. Multicenter randomized controlled trial of intensive uric acid lowering therapy for CKD patients with hyperuricemia: TARGET-UA. Clin Exp Nephrol. 2024 Aug;28(8):764-772. doi: 10.1007/s10157-024-02483-w. Epub 2024 Mar 26. PMID: 38530491; PMCID: PMC11266370. 11: Kuwabara M, Nakai M, Sumita Y, Iwanaga Y, Ae R, Kodama T, Hisatome I, Kamatani N. Xanthine oxidase inhibitors treatment or discontinuation effects on mortality: evidence of xanthine oxidase inhibitors withdrawal syndrome. Front Pharmacol. 2024 Jan 8;14:1289386. doi: 10.3389/fphar.2023.1289386. PMID: 38259292; PMCID: PMC10800388. 12: Takayama A, Fukasawa T, Takeuchi M, Kawakami K. Timing of Initiation of Xanthine Oxidase Inhibitors Based on Serum Uric Acid Level Does Not Predict Renoprognosis in Patients with Preserved Kidney Function. Metab Syndr Relat Disord. 2024 Apr;22(3):222-231. doi: 10.1089/met.2023.0238. Epub 2024 Jan 3. PMID: 38170182. 13: Singh A, Singh K, Sharma A, Kaur K, Chadha R, Singh Bedi PM. Past, present and future of xanthine oxidase inhibitors: design strategies, structural and pharmacological insights, patents and clinical trials. RSC Med Chem. 2023 Aug 7;14(11):2155-2191. doi: 10.1039/d3md00316g. PMID: 37974965; PMCID: PMC10650961. 14: Mitsuboshi S, Morizumi M, Kotake K, Kaseda R, Narita I. Urate-Lowering Drugs and Muscle Injury: A Systematic Review and Network Meta-Analysis. J Clin Pharmacol. 2024 Mar;64(3):288-299. doi: 10.1002/jcph.2369. Epub 2023 Oct 30. PMID: 37840156. 15: Maghsoud Y, Dong C, Cisneros GA. Computational Characterization of the Inhibition Mechanism of Xanthine Oxidoreductase by Topiroxostat. ACS Catal. 2023 May 5;13(9):6023-6043. doi: 10.1021/acscatal.3c01245. Epub 2023 Apr 18. PMID: 37547543; PMCID: PMC10399974. 16: Fujishima Y, Nishizawa H, Kawachi Y, Nakamura T, Akari S, Ono Y, Fukuda S, Kita S, Maeda N, Hoshide S, Shimomura I, Kario K. The Effects of Topiroxostat, a Selective Xanthine Oxidoreductase Inhibitor, on Arterial Stiffness in Hyperuricemic Patients with Liver Dysfunction: A Sub-Analysis of the BEYOND-UA Study. Biomedicines. 2023 Feb 23;11(3):674. doi: 10.3390/biomedicines11030674. PMID: 36979653; PMCID: PMC10045538. 17: Hu SS, Zhang TJ, Wang ZR, Xu EY, Wang QY, Zhang X, Guo S, Ge GH, Wang J, Meng FH. Design, synthesis and structure-activity relationship of N-phenyl aromatic amide derivatives as novel xanthine oxidase inhibitors. Bioorg Chem. 2023 Apr;133:106403. doi: 10.1016/j.bioorg.2023.106403. Epub 2023 Feb 3. PMID: 36801790. 18: Naganuma J, Sakuma M, Kitahara K, Kato T, Yokomachi J, Yamauchi F, Inoue R, Iida K, Kohno Y, Inoue K, Koshiji N, Abe S, Toyoda S, Inoue T; Excited UA study investigators. Optimal uric acid reduction to improve vascular endothelial function in patients with chronic heart failure complicated by hyperuricemia. Hypertens Res. 2023 Mar;46(3):688-696. doi: 10.1038/s41440-022-01116-7. Epub 2022 Dec 20. PMID: 36539463. 19: Noda M, Kikuchi C, Tarui R, Nakamura T, Murase T, Hori E, Matsunaga T. Effect of Topiroxostat on Reducing Oxidative Stress in the Aorta of Streptozotocin-Induced Diabetic Rats. Biol Pharm Bull. 2023 Feb 1;46(2):272-278. doi: 10.1248/bpb.b22-00694. Epub 2022 Dec 16. PMID: 36529499. 20: Sawada S, Kajiyama K, Shida H, Kimura R, Nakazato Y, Iguchi T, Oniyama Y, Ishiguro C, Uyama Y. Cardiovascular risk of urate-lowering drugs: A study using the National Database of Health Insurance Claims and Specific Health Checkups of Japan. Clin Transl Sci. 2023 Feb;16(2):206-215. doi: 10.1111/cts.13439. Epub 2022 Nov 11. PMID: 36317407; PMCID: PMC9926079.