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3-aminobenzamide

 
Catalog No.
A4161
强效的PARP抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 454.00
现货
250mg
¥ 454.00
现货
500mg
¥ 690.00
现货

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A

背景

3-Aminobenzamide (PARP-IN-1)是一种有效的 PARP 抑制剂,在CHO细胞中,对PARP的IC50值约为50nM,并在再灌注过程中充当氧化剂诱导的心肌细胞功能障碍的介质。

3-Aminobenzamide (PARP-IN-1) (>1 μM)对95%以上PARP活性有抑制作用,但没有明显的细胞毒性。3-Aminobenzamide在暴露于400μM H2O2后通过增强乙酰胆碱诱导的内皮依赖性一氧化氮介导的血管舒张作用显着改善内皮功能[1]

在db/db(Leprdb / db)小鼠模型中,3-Aminobenzamide改善了糖尿病引起的白蛋白排泄和肾小球系膜扩张,并减少了糖尿病引起的足细胞消耗[2]

[1]. Radovits T, et al. Poly (ADP-ribose) polymerase inhibition improves endothelial dysfunction induced by reactive oxidant hydrogen peroxide in vitro. Eur J Pharmacol. 2007 Jun 14;564(1-3):158-66.

[2]. Szabo C, et al. Poly (ADP-ribose) polymerase inhibitors ameliorate nephropathy of type 2 diabetic Leprdb/db mice. Diabetes. 2006 Nov;55(11):3004-12.

文献引用

1. Grunewald ME, Chen Y, et al. "The coronavirus macrodomain is required to prevent PARP-mediated inhibition of virus replication and enhancement of IFN expression." PLoS Pathog. 2019 May 16;15(5):e1007756. PMID:31095648
2. Waldman M, Nudelman V, et al. "PARP-1 inhibition protects the diabetic heart through activation of SIRT1-PGC-1α axis." Exp Cell Res. 2018 Oct 23. pii: S0014-4827(18)31064-4. PMID:30359575

化学属性

Physical AppearanceA solid
StorageStore at -20°C
M.Wt136.15
Cas No.3544-24-9
FormulaC7H8N2O
SynonymsPARP-IN-1
Solubility≥23.45 mg/mL in H2O with ultrasonic; ≥48.1 mg/mL in EtOH with ultrasonic; ≥7.35 mg/mL in DMSO
Chemical Name3-aminobenzamide
SDFDownload SDF
Canonical SMILESC1=CC(=CC(=C1)N)C(=O)N
运输条件 蓝冰运输或根据您的需求运输。
一般建议不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

生物活性

3-aminobenzamide is a potent inhibitor of PARP with IC50 of <50 nM in CHO cells and a mediator of oxidant-induced myocyte dysfunction during reperfusion. Phase 2.
Targets PARP          
IC50 50 nM          

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