1. Metabolic Enzyme/Protease
  2. Xanthine Oxidase
  3. Topiroxostat

Topiroxostat (Synonyms: FYX-051)

Cat. No.: HY-14874 Purity: 98.54%
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Topiroxostat(FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM.

For research use only. We do not sell to patients.

Topiroxostat Chemical Structure

Topiroxostat Chemical Structure

CAS No. : 577778-58-6

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10 mM * 1 mL in DMSO USD 66 In-stock
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50 mg USD 190 In-stock
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200 mg USD 480 In-stock
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Based on 2 publication(s) in Google Scholar

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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 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].

Clinical Trial
Molecular Weight

248.24

Formula

C₁₃H₈N₆

CAS No.

577778-58-6

SMILES

N#CC1=NC=CC(C2=NNC(C3=CC=NC=C3)=N2)=C1

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Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 23.5 mg/mL (94.67 mM; Need ultrasonic and warming)

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Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0284 mL 20.1418 mL 40.2836 mL
5 mM 0.8057 mL 4.0284 mL 8.0567 mL
10 mM 0.4028 mL 2.0142 mL 4.0284 mL
*Please refer to the solubility information to select the appropriate solvent.
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Topiroxostat
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