Topiroxostat (FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM. Topiroxostat (FYX-051) exhibited competitive-type inhibition with a Ki value of 5.7 × 10-9 M of native XO.
In vivo: In this hyperuricemic model, Topiroxostat in the dose range of 0.03 to 1 mg/kg 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.
| Molecular Weight | 248.24 |
| Formula | C13H8N6 |
| CAS Number | 577778-58-6 |
| Form | Solid |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Xanthine Oxidase Products |
|---|
| H-Tyr-Phe-OH
H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. |
| TEI-6469
TEI-6469 is a xanthine oxidase (XO) inhibitor that may be used in studies related to gout. |
| Phytic acid dodecasodium hydrate
Phytic acid (Inositol hexaphosphate) dodecasodium hydrate is a phosphorus storage compound of seeds and cereal grains. |
| Ellagic acid-4-O-beta-D-xylopyranoside
Ellagic acid 4-O-β-D-xylopyranoside is a natural ellagitannin with antimicrobial activity. Ellagic acid 4-O-β-D-xylopyranoside is an xanthine oxidase inhibitor with an 50 of 2.1 μg/mL. |
| Protosappanin A dimethyl acetal
Protosappanin A dimethyl acetal is a homoisoflavonoid. |
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