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Picolinamide

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Chemical Structure| 1452-77-3 同义名 : 2-吡啶甲酰胺 ;2-Picolinamide;2-Pyridinecarboxamide;2-Carbamoylpyridine;Picolinoylamide
CAS号 : 1452-77-3
货号 : A226558
分子式 : C6H6N2O
纯度 : 98%
分子量 : 122.125
MDL号 : MFCD00023483
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(409.42 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(818.84 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • PARP

    PARP, IC50:95 μM
描述 Picolinamide was found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells[3]. Picolinamide was used in the present study to explore the possibility that inhibition of Na+/phosphate cotransport may be related to inhibition of NAD hydrolyzing enzymes. Overnight treatment of rats with picolinamide, administered as a single injection (4 mmol/kg), inhibited Na+/phosphate cotransport by isolated renal brush border membrane vesicles[4]. Picolinamide (250 mg/kg, i.p., rats) enhances the tumorigenic effect of Streptozotocin and Alloxan on islet B-cells[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03033485 Melanoma Not Applicable Not yet recruiting December 2018 China, Shaanxi ... 展开 >> Xijing Hospital Nuclear Medicine Department Xi'an, Shaanxi, China, 710032 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

8.19mL

1.64mL

0.82mL

40.94mL

8.19mL

4.09mL

81.88mL

16.38mL

8.19mL
参考文献

[1]Campbell PI, al-Mahrouq HA, et al. Specific inhibition of rat renal Na+/phosphate cotransport by picolinamide. J Pharmacol Exp Ther. 1989 Oct;251(1):188-92.

[2]Orpin CG, Knight M, Evans WC. The bacterial oxidation of picolinamide, a photolytic product of Diquat. Biochem J. 1972 May;127(5):819-31.

[3]Uchigata Y, Yamamoto H, Kawamura A, Okamoto H. Protection by superoxide dismutase, catalase, and poly(ADP-ribose) synthetase inhibitors against alloxan- and streptozotocin-induced islet DNA strand breaks and against the inhibition of proinsulin synthesis. J Biol Chem. 1982;257(11):6084-6088.

[4]Campbell PI, al-Mahrouq HA, Abraham MI, Kempson SA. Specific inhibition of rat renal Na+/phosphate cotransport by picolinamide. J Pharmacol Exp Ther. 1989;251(1):188-192.

[5]Yamagami T, Miwa A, Takasawa S, Yamamoto H, Okamoto H. Induction of rat pancreatic B-cell tumors by the combined administration of streptozotocin or alloxan and poly(adenosine diphosphate ribose) synthetase inhibitors. Cancer Res. 1985;45(4):1845-1849.