577778-58-6 Topirox...

577778-58-6 Topiroxostat

577778-58-6 Topiroxostat

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1 Gram

FOB Price: USD 8000.0000

  • Min.Order :1 Gram
  • Purity: 98%min
  • Payment Terms : T/T,

Keywords

Topiroxostat FYX-051 577778-58-6

Quick Details

  • Appearance: light white or white powder
  • Application:Research purpose
  • PackAge:1kg/Aluminum foil bag
  • ProductionCapacity:500|Kilogram|Month
  • Storage: Kept in a cool, dry and ventilated place
  • Transportation:by air

Superiority:

Topiroxostat 

Another name: FYX-051

CasNo: 577778-58-6

M.Wt: 248.24

Formula: C13H8N6

Solubility:DMSO

Appearance: light white or white powder

Application: Use as the pharma

Purity: 99%

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 oxidoreductase
in 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].

Details:

Topiroxostat 

Another name: FYX-051

CasNo: 577778-58-6

M.Wt: 248.24

Formula: C13H8N6

Solubility:DMSO

Appearance: light white or white powder

Application: Use as the pharma

Purity: 99%

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 oxidoreductase
in 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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