Topiroxostat

China [CN]

I. Basic Information

Item | Details

English Name | Topiroxostat; FYX-051; TOPILORIC (Trade Name)

Chinese Name | Topiroxostat

CAS Number | 577778-58-6

Chemical Name | 5-(2-cyano-4-pyridinyl)-3-(4-pyridinyl)-1,2,4-triazole

Molecular Formula | C₁₃H₈N₆

Molecular Weight | 248.25

Target | Xanthine oxidoreductase (XOR, IC₅₀=5.3 nM, Ki=5.7 nM)

Developing Company | Fuji Yakuhin Co., Ltd. (Japan)

Market Launch Date | June 2013 (Japan PMDA); Not yet launched in China

Dosage Form and Strength | Tablets: 20mg, 40mg, 60mg

II. Physicochemical Properties

Parameter | Data

Appearance | White to pale yellow crystalline powder

Solubility | Slightly soluble in water, soluble in dimethyl sulfoxide (DMSO), N,N-dimethylformamide, sparingly soluble in ethanol and diethyl ether

Dissociation Constant (pKa) | Approximately 4.8 (pyridine ring), approximately 9.2 (triazole ring) (predicted value)

Melting Point | 212℃ (decomposition)

Stability | Stable for 24 months at 25℃/60% RH, store in a sealed container in a cool, dry place, avoid high temperature, light and moisture

Partition Coefficient (logP) | 2.3 (predicted value)

Chiral Characteristics | No chiral center, single structure