1-[3-CYANO-4-(2,2-DIMETHYL-PROPOXY)-PHENYL]-1H-PYRAZOLE-4-CARBOXYLIC ACID
1-[3-CYANO-4-(2,2-DIMETHYL-PROPOXY)-PHENYL]-1H-PYRAZOLE-4-CARBOXYLIC ACID Basic information
- Product Name:
- 1-[3-CYANO-4-(2,2-DIMETHYL-PROPOXY)-PHENYL]-1H-PYRAZOLE-4-CARBOXYLIC ACID
- Synonyms:
-
- 1-[3-CYANO-4-(2,2-DIMETHYL-PROPOXY)-PHENYL]-1H-PYRAZOLE-4-CARBOXYLIC ACID
- 1H-PYRAZOLE-4-CARBOXYLIC ACID, 1-[3-CYANO-4-(2,2-DIMETHYLPROPOXY)PHENYL]-
- PIRAXOSTAT
- Y 700
- Niraxostat
- AETHRPHBGJAIBT-UHFFFAOYSA-N
- Y 700 - Piraxostat
- 1-(3-cyano-4-(neopentyloxy)phenyl)-1H-pyrazole-4-carboxylic acid
- CAS:
- 206884-98-2
- MF:
- C16H17N3O3
- MW:
- 299.32
- Mol File:
- 206884-98-2.mol
1-[3-CYANO-4-(2,2-DIMETHYL-PROPOXY)-PHENYL]-1H-PYRAZOLE-4-CARBOXYLIC ACID Chemical Properties
- Boiling point:
- 500.5±45.0 °C(Predicted)
- Density
- 1.20±0.1 g/cm3(Predicted)
- pka
- 3.68±0.10(Predicted)
- form
- Solid
- color
- White to off-white
1-[3-CYANO-4-(2,2-DIMETHYL-PROPOXY)-PHENYL]-1H-PYRAZOLE-4-CARBOXYLIC ACID Usage And Synthesis
Uses
Niraxostat (Y-700; Piraxostat) is an orally active xanthine oxidoreductase (XOR) inhibitor used in the study of hyperuricemia and other diseases in which XOR may be involved[1].
in vivo
Niraxostat (Y-700; 1 mg/kg) has high oral bioavailability (84.1%) and is almost not excreted through the kidneys. It is mainly eliminated through the liver[1].
Niraxostat (Y- 700; 1-10 mg/kg; oral; single dose) dose-dependently reduces plasma urate levels in oxonate-treated rats [1].
Niraxostat (Y-700 ; 0.3-3 mg/kg; Oral; Single dose) In normal rats, dose-dependently reduces urinary excretion of urate and allantoin while increasing excretion of hypoxanthine and xanthine [1].
Pharmacokinetic Analysis of Niraxostat (Y-700) in normal rats[1]
| Route | Dose (mg/kg) | tmax (h) | Cmax (μg/ml) | AUC0-∞ (μg/h/ml) | t1/2 (h) |
| PO | 0.3 | 0.5 | 0.43 | 2.07 | 5.0 |
| PO | 1 | 0.3 | 1.8 | 7.01 | 3.2 |
| PO | 3 | 0.5 | 6.49 | 30.31 | 2.7 |
| IV | 1 | / | 3.97 | 8.34 | 2.5 |
References
[1] Fukunari A, et al. Y-700 [1-[3-Cyano-4-(2,2-dimethylpropoxy)phenyl]-1H-pyrazole-4-carboxylic acid]: a potent xanthine oxidoreductase inhibitor with hepatic excretion. J Pharmacol Exp Ther. 2004 Nov;311(2):519-28. DOI:10.1124/jpet.104.070433
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