Name: Picolinamide
Price: 180.00 USD

- Overview
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    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.
    
    [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.
- Properties
  - Alternative Name
    
    picolinamide
    
    CAS Number
    
    1452-77-3
    
    Molecular Formula
    
    C6H6N2O
    
    Molecular Weight
    
    122.12
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥83.33 mg/mL in DMSO; insoluble in H2O; ≥14.54 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Picolinamide

Picolinamide

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