577778-58-6
577778-58-6 structure
- Name: Topiroxostat
- Chemical Name: 4-(5-pyridin-4-yl-1H-1,2,4-triazol-3-yl)pyridine-2-carbonitrile
- CAS Number: 577778-58-6
- Molecular Formula: C13H8N6
- Molecular Weight: 248.243
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Xanthine Oxidase
- Create Date: 2018-03-24 08:00:00
- Modify Date: 2026-07-02 08:29:29
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Topiroxostat(FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM.IC50 value: 5.3 nM [1]Target: xanthine oxidoreductasein vitro: Steady-state kinetics study showed that FYX-051 initially behaved as a competitive-type inhibitor with a K(i) value of 5.7 × 10(-9) M, then after a few minutes it formed a tight complex with XOR via a Mo-oxygen-carbon atom covalent linkage, as reported previously [3].in vivo: FYX-051 exhibited a weak CYP3A4-inhibitory activity (18.6%); its Cmax and bioavailability were as high as 4.62 μg/mL (3 mg/kg) and 69.6%, respectively. Moreover, the t1/2 value of 39 was greater (19.7 h) than that of compound 2 (0.97 h) [1]. In the mechanistic study by 52-week oral treatment with topiroxostat at 3 mg/kg to F344 male rats, with and without citrate, simple and papillary transitional cell hyperplasias of the urinary bladder epithelium were observed in 5/17 in the topiroxostat-alone treatment group, along with xanthine-induced nephropathy, in contrast to neither xanthine crystals nor lesions in urinary organs by co-treatment group with citrate [2].
| Name | 4-(5-pyridin-4-yl-1H-1,2,4-triazol-3-yl)pyridine-2-carbonitrile |
|---|---|
| Synonyms |
3-(3-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole
Topiroxostat,FYX-051 5-(2-Cyano-4-pyridyl)-3-(4-pyridyl)-1,2,4-triazole Uriadec (TN) Toby Str [14C]-Topiroxostat 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile FYX-051; FYX051; FYX 051; TOPIROXOSTAT. TRADE NAMES TOPILORIC; URIADEC 4-[5-(4-pyridinyl)-1H-1,2,4-triazol-3-yl]-2-Pyridinecarbonitrile Topiroxostat. trade names Topiloric 4-[5-(4-Pyridyl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile Topiester N-desmethyl N-Nitroso Topotecan-D3 Uriadec 4-(5-(pyridin-4-yl)-1h-1,2,4-triazol-3-yl)picolinonitrile Topiroxostat C13H8N6 high quality Cas number：577-6 Topiroxostat, 10 mM in DMSO 4-[3-(4-Pyridinyl)-1H-1,2,4-triazol-5-yl]-2-pyridinecarbonitrile FYX 051 D4-Topiroxostat 4-(3-(Pyridin-4-yl)-1H-1,2,4-triazol-5-yl)picolinonitrile 4-(3-(Pyridin-4-yL 4-[5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile Topicast impurity Topiroxosta Topiloric Topiroxostat [INN] 2-Pyridinecbonitrile, 4-[5-(4-pyridinyl)-1H-1,2,4-triazol-3-yl] Topiroxostat impurty Topiroxostat 5-(2-Cyano-4-pyridyl)-3-(4-pyridyl)-1,2,4-triazole 2-Pyridinecbonitrile, 4-[3-(4-pyridinyl)-1H-1,2,4-triazol-5-yl] Factory supply Topiroxostat Cas 577-6 with high quality and best price inonitriL |
| Description | Topiroxostat(FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM.IC50 value: 5.3 nM [1]Target: xanthine oxidoreductasein vitro: Steady-state kinetics study showed that FYX-051 initially behaved as a competitive-type inhibitor with a K(i) value of 5.7 × 10(-9) M, then after a few minutes it formed a tight complex with XOR via a Mo-oxygen-carbon atom covalent linkage, as reported previously [3].in vivo: FYX-051 exhibited a weak CYP3A4-inhibitory activity (18.6%); its Cmax and bioavailability were as high as 4.62 μg/mL (3 mg/kg) and 69.6%, respectively. Moreover, the t1/2 value of 39 was greater (19.7 h) than that of compound 2 (0.97 h) [1]. In the mechanistic study by 52-week oral treatment with topiroxostat at 3 mg/kg to F344 male rats, with and without citrate, simple and papillary transitional cell hyperplasias of the urinary bladder epithelium were observed in 5/17 in the topiroxostat-alone treatment group, along with xanthine-induced nephropathy, in contrast to neither xanthine crystals nor lesions in urinary organs by co-treatment group with citrate [2]. |
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| Related Catalog | |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 594.7±60.0 °C at 760 mmHg |
| Molecular Formula | C13H8N6 |
| Molecular Weight | 248.243 |
| Flash Point | 175.3±18.1 °C |
| Exact Mass | 248.081039 |
| PSA | 91.14000 |
| LogP | 1.35 |
| Vapour Pressure | 0.0±1.7 mmHg at 25°C |
| Index of Refraction | 1.697 |
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577778-58-6 |
| Literature: EP1471065 A1, ; Page 8 ; |
| Precursor 2 | |
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| DownStream 0 | |