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Picolinamide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Picolinamide图片
CAS NO:1452-77-3
规格:98%
分子量:122.12
包装与价格:
包装价格(元)
100mg电议
500mg电议

产品介绍
poly (ADP-ribose) synthetase inhibitor
CAS:1452-77-3
分子式:C6H6N2O
分子量:122.12
纯度:98%
存储:Store at -20°C

Background:

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 [1].


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 [2].


Clinical trial: Up to now, picolinamide is still in the preclinical development stage.


参考文献:
[1] C.  G. Orpin,M. Knight, and W. C. Evans. The bacterial oxidation of picolinamide, a photolytic product of DiquatBiochem J. 1972 May; 127(5): 819–831.
[2] Campbell PI, al-Mahrouq HA,Abraham MI,Kempson SA.  Specific inhibition of rat renal Na+/phosphate cotransport by picolinamide. J Pharmacol Exp Ther.1989 Oct;251(1):188-92.