Application
一种具有PARP抑制活性的烟酸胺肟衍生物。
As a group of pharmacological inhibitors of the enzyme poly ADP ribose polymerase(PARP), PARP inhibitors are considered a potential treatment for stroke and myocardial infarction.
In vitro: Previous study showed that BGP-15 at 200 μM could prevent the imatinib-induced oxidative damages, attenuate the depletion of high-energy phosphates, alter the signaling effect of imatinib by preventing p38 MAP kinase and JNK activation, and also induce the Akt and GSK-3β phosphorylation
In vivo: In-vivo study indicated that BGP-15 improved cardiac function and reduced arrhythmic episodes in two HF and AF mouse models. In these models, BGP-15 was associated with increased phosphorylation of IGF1R. Moreover, cardiac-specific IGF1R transgenic overexpression in mice recapitulated the protection caused by BGP-15. The authors further demonstrated that BGP-15 with IGF1R could provide protection independent of phosphoinositide 3-kinase-Akt and heat-shock protein 70.
作为多聚ADP核糖聚合酶（PARP）酶的药理抑制剂，PARP抑制剂被认为是中风和心肌梗塞的潜在治疗方法。
体外：先前的研究表明，200μM的BGP-15可以预防伊马替尼诱导的氧化损伤，减弱高能磷酸盐的消耗，通过防止p38 MAP激酶和JNK活化来改变伊马替尼的信号传导作用，并诱导 Akt和GSK-3β磷酸化
体内：体内研究表明，在两种HF和AF小鼠模型中，BGP-15改善了心脏功能，并减少了心律失常发作。 在这些模型中，BGP-15与IGF1R的磷酸化增加有关。 此外，小鼠心脏特异性IGF1R转基因过表达概括了由BGP-15引起的保护作用。 作者进一步证明，带有IGF1R的BGP-15可以提供独立于磷酸肌醇3激酶-Akt和热休克蛋白70的保护。
性质
| Iupac Name | N-(2-hydroxy-3-(piperidin-1-yl)propoxy)nicotinimidamide dihydrochloride |
| Inchi Code | 1S/C14H22N4O2.2ClH/c15-14(12-5-4-6-16-9-12)17-20-11-13(19)10-18-7-2-1-3-8-18;;/h4-6,9,13,19H,1-3,7-8,10-11H2,(H2,15,17);2*1H |
| Inchi Key | ISGGVCWFTPTHIX-UHFFFAOYSA-N |
安全信息
RIDADR NONH for all modes of transport
