Picolinamide
(Synonyms:2-吡啶甲酰胺;吡啶-2-甲酰胺;2-吡啶酰胺;吡啶酰胺;2-Picolinamide 2-吡啶酰胺;2-酰氨基吡啶;吡啶酰胺: PYRIDINE-2-CARBOXAMIDE;吡啶酰胺 5G;吡啶-2-甲酰胺,98%)
目录号 : KG10916
CAS No. : 1452-77-3
纯度 : 98%
Picolinamide is a poly (ADP-ribose) synthetase (PARP) inhibitor.
PARP inhibitors, a group of pharmacological inhibitors of the enzyme poly ADP ribose polymerase (PARP), are developed for multiple indications, especially for the treatment of cancer.
In vitro: The pathway of oxidation of picolinamide by a Gram-negative rod has been elucidated. Results showed that under high pH conditions, whole cells could release 2,5-dihydroxypyridine into culture supernatants. Moreover, sodium arsenite was able to cause whole cells to accumulate 6-hydroxypicolinate in the culture media. In addition, whole cells were found to oxidize picolinamide, without lag. It was also found that cell-free extracts could convert picolinamide into picolinate, and hydroxylate picolinate into 6-hydroxypicolinate .
In vivo: Picolinamide was used in a previous study to evaluate the possibility that the inhibition of Na+/phosphate cotransport might be associated with the inhibition of NAD hydrolyzing enzymes. Results showed that the overnight treatment of rats with picolinamide, administered as a single injection (4 mmol/kg), could inhibit Na+/phosphate cotransport by isolated renal brush border membrane vesicles. Similar to nicotinamide, the inhibition caused by picolinamide occurred in thyroparathyroidectomized rats, was specific for Na+/phosphate cotransport. Unlike nicotinamide, there was only a small 1.5-fold increase in renal cortical NAD content after picolinamide treatment .
Clinical trial: Up to now, picolinamide is still in the preclinical development stage.
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| 分子式 |
C6H6N2O
|
| 分子量 |
122.12
|
| CAS号 |
1452-77-3
|
| 中文名称 |
2-吡啶甲酰胺
|
| 储存方式 |
| Powder |
-20°C |
3 years |
| |
4°C |
2 years |
| In solvent |
-80°C |
6 months |
| |
-20°C |
1 month |
|