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吡啶酰胺 /Picolinamide {[allProObj[0].p_purity_real_show]}

货号:A226558 同义名: 2-吡啶甲酰胺 / 2-Picolinamide;2-Pyridinecarboxamide

Picolinamide is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells.

Picolinamide 化学结构 CAS号:1452-77-3
Picolinamide 化学结构
CAS号:1452-77-3
Picolinamide 3D分子结构
CAS号:1452-77-3
Picolinamide 化学结构 CAS号:1452-77-3
Picolinamide 3D分子结构 CAS号:1452-77-3
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Picolinamide 纯度/质量文件 产品仅供科研

货号:A226558 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 PARP PARP1 PARP2 PARP3 其他靶点 纯度
PJ34 HCl ++

PARP, EC50: 20 nM

99%+
Rucaparib phosphate ++++

PARP, Ki: 1.4 nM

99%+
3-Aminobenzamide ++

PARP, IC50: <50 nM

98%
AZD-2461 99%+
BGP-15 99%+
NU1025 +

PARP, IC50: 400 nM

97%
Benzamide +

PARP, IC50: 3.3 μM

98%
Picolinamide +

PARP, IC50: 95 μM

98%
AG14361 +++

PARP1, Ki: <5 nM

98+%
Iniparib 98%
Talazoparib ++++

PARP1, IC50: 0.57 nM

99%+
NMS-P118 ++

PARP1, Kd: 0.009 μM

98+%
UPF 1069 +

PARP1, IC50: 8.0 μM

++

PARP2, IC50: 0.3 μM

98%
A-966492 ++++

PARP1, EC50: 1 nM

PARP1, Ki: 1 nM

+++

PARP2, Ki: 1.5 nM

99%+
Veliparib ++

PARP1, Ki: 5.2 nM

+++

PARP2, Ki: 2.9 nM

98%
Niraparib tosylate +++

PARP1, IC50: 3.8 nM

+++

PARP2, IC50: 2.1 nM

99%+
Stenoparib ++++

PARP1, IC50: 1 nM

++++

PARP2, IC50: 1.2 nM

98%
Olaparib +++

PARP1, IC50: 5 nM

++++

PARP2, IC50: 1 nM

98%
Niraparib +++

PARP1, IC50: 3.8 nM

+++

PARP2, IC50: 2.1 nM

98%
ME0328 +

PARP1, IC50: 6.3 μM

+

PARP3, IC50: 0.89 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Picolinamide 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].

Picolinamide 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 <<

Picolinamide 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.

Picolinamide 实验方案

计算器
存储液制备 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

Picolinamide 技术信息

CAS号1452-77-3
分子式C6H6N2O
分子量 122.125
别名 2-吡啶甲酰胺 ;2-Picolinamide;2-Pyridinecarboxamide;2-Carbamoylpyridine;Picolinoylamide
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

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
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