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product name Picolinamide


Description: Picolinamide (2-Pyridinecarboxamide, Picolinoylamide, 2-Carbamoylpyridine) is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells. 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 could inhibit Na+/phosphate cotransport by isolated renal brush border membrane vesicles.

References: Cancer Res. 1985;45(4):1845-9; J Biol Chem. 1982;257(11):6084-8; J Pharmacol Exp Ther. 1989;251(1):188-92.



Molecular Weight (MW)

122.12 
Formula

C6H6N2
CAS No.

1452-77-3 
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 24 mg/mL (196.5 mM) 
Water: 24 mg/mL (196.5 mM) 
Ethanol: 24 mg/mL (196.5 mM) 
Solubility (In vivo)

 
Synonyms

2-Pyridinecarboxamide, Picolinoylamide, 2-Carbamoylpyridine 

other peoduct :

In Vitro

In vitro activity: Overnight treatment of rats with picolinamide, administered as a single injection (4 mmol/kg), inhibits Na+/phosphate cotransport by isolated renal brush border membrane vesicles. There is only a small increase (1.5-fold) in renal cortical NAD content after picolinamide treatment.


Kinase Assay:


Cell Assay: 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. 
Animal model Wistar rats 
Formulation & Dosage Dissolved in 0.9% NaCl solution; 250 mg/kg; i.p. injection
References Cancer Res. 1985 Apr;45(4):1845-9; J Biol Chem. 1982 Jun 10;257(11):6084-8; J Pharmacol Exp Ther. 1989 Oct;251(1):188-92. 

AXL1719

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Author: Sodium channel