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Picolinamide

Catalog No.GC14251

poly (ADP-ribose) synthetase inhibitor

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Picolinamide Chemical Structure

Cas No.: 1452-77-3

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10mM (in 1mL DMSO)
$37.00
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100mg
$50.00
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500mg
$143.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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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.

References:
[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.

Chemical Properties

Cas No. 1452-77-3 SDF
Chemical Name picolinamide
Canonical SMILES NC(C1=CC=CC=N1)=O
Formula C6H6N2O M.Wt 122.12
Solubility ≥ 83.3mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 8.1887 mL 40.9433 mL 81.8867 mL
5 mM 1.6377 mL 8.1887 mL 16.3773 mL
10 mM 0.8189 mL 4.0943 mL 8.1887 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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