Topiroxostat
Based on 8 publication(s) in Google Scholar
Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.06%
- No. CAS: 577778-58-6
- Fòrmula: C13H8N6
- Peso molecular:248.24
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Topiroxostat
More- Cancer Cell. 2023 Feb 13;41(2):356-372.e10. [Abstract]
- Cell Host Microbe. 2026 Jun 3:S1931-3128(26)00181-2. [Abstract]
- Nat Commun. 2020 Jun 2;11(1):2767. [Abstract]
- J Am Heart Assoc. 2021 Dec 7;10(23):e022712. [Abstract]
- Front Pharmacol. 2016 Dec 27:7:518. [Abstract]
- Molecules. 2026 Mar 5;31(5):864. [Abstract]
- Expert Opin Ther Targets. 2016;20(3):375-87. [Abstract]
- Patent. US20250263496A1.
Actividad biológica
Descripciòn
IC50 & Target
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CYP3 |
In Vitro
These potent and more sustained effects of Topiroxostat (FYX-051, compound 39) have been confirmed by a crystallographic analysis of XOR-Topiroxostat complex. The cyano group of Topiroxostat has been reported to play an important role in the binding activity between Topiroxostat and XOR. This is attributable to the formation of a hydrogen bond between Asn 768 of XOR and the cyano group of Topiroxostat[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
The Cmax and bioavailability of Topiroxostat (FYX-051, compound 39) are as high as 4.62 μg/mL (3 mg/kg) and 69.6%, respectively. Moreover, the t1/2 value of Topiroxostat is 19.7 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar/ST strain rats (7 weeks old) injected with potassium oxonate[2]
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Dosage:0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg
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Administration:Oral administration; for 1 hour
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Result:Caused a dose-dependent decrease in serum urate levels with an extremely low ED50 of 0.15 mg/kg, evaluated at 1 h after oral administration.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 577778-58-6
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Appearance Solid
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Peso molecular 248.24
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Fòrmula C13H8N6
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Color White to off-white
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SMILES
N#CC1=NC=CC(C2=NNC(C3=CC=NC=C3)=N2)=C1
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Synonyms
FYX-051
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Cancer Cell
2023 Feb 13;41(2):356-372.e10. PMID: 36706760 -
Cell Host Microbe
Uric acid promotes dietary lipid absorption through microbiome and metabolomic remodeling via a liver-gut endocrine axis. [Abstract]2026 Jun 3:S1931-3128(26)00181-2. PMID: 42235504 -
Nat Commun
The ABCG2 Q141K hyperuricemia and gout associated variant illuminates the physiology of human urate excretion. [Abstract]2020 Jun 2;11(1):2767. PMID: 32488095 -
J Am Heart Assoc
2021 Dec 7;10(23):e022712. PMID: 34845934 -
Front Pharmacol
Identification of Febuxostat as a New Strong ABCG2 Inhibitor: Potential Applications and Risks in Clinical Situations. [Abstract]2016 Dec 27:7:518. PMID: 28082903 -
Molecules
2026 Mar 5;31(5):864. PMID: 41828851 -
Expert Opin Ther Targets
2016;20(3):375-87. PMID: 26419119 -
Solvente y solubilidad
In Vitro:
DMSO : 23.5 mg/mL (94.67 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Sato T, et al. Discovery of 3-(2-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051 - a xanthine oxidoreductase inhibitor for the treatment of hyperuricemia [corrected]. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6225-9. [Content Brief]
[2]. Matsumoto K, et al. FYX-051: a novel and potent hybrid-type inhibitor of xanthine oxidoreductase. J Pharmacol Exp Ther. 2011 Jan;336(1):95-103. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.0284 mL | 20.1418 mL | 40.2836 mL | 100.7090 mL |
| 5 mM | 0.8057 mL | 4.0284 mL | 8.0567 mL | 20.1418 mL | |
| 10 mM | 0.4028 mL | 2.0142 mL | 4.0284 mL | 10.0709 mL | |
| 15 mM | 0.2686 mL | 1.3428 mL | 2.6856 mL | 6.7139 mL | |
| 20 mM | 0.2014 mL | 1.0071 mL | 2.0142 mL | 5.0354 mL | |
| 25 mM | 0.1611 mL | 0.8057 mL | 1.6113 mL | 4.0284 mL | |
| 30 mM | 0.1343 mL | 0.6714 mL | 1.3428 mL | 3.3570 mL | |
| 40 mM | 0.1007 mL | 0.5035 mL | 1.0071 mL | 2.5177 mL | |
| 50 mM | 0.0806 mL | 0.4028 mL | 0.8057 mL | 2.0142 mL | |
| 60 mM | 0.0671 mL | 0.3357 mL | 0.6714 mL | 1.6785 mL | |
| 80 mM | 0.0504 mL | 0.2518 mL | 0.5035 mL | 1.2589 mL |
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