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BGP-15

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Chemical Structure| 66611-37-8 同义名 : BGP-15 2HCl
CAS号 : 66611-37-8
货号 : A202611
分子式 : C14H24Cl2N4O2
纯度 : 99%+
分子量 : 351.272
MDL号 : MFCD21603901
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 10 mg/mL(28.47 mM)，配合低频超声，并水浴加热至45℃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(284.68 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • PARP
描述 Poly(ADP-ribose) polymerase-1 (PARP1) and poly(ADP-ribose) polymerase-2 (PARP2), members of the PARP superfamily of enzymes, play a key role in DNA damage response (DDR) by acting as DNA damage sensors and signal transducers. In a process known as poly-ADP-ribosylation (PARylation), PARP1 transfers ADP-ribose from nicotinamide adenine dinucleotide (NAD+) to target proteins, which in turn enables recruitment of DNA repair proteins[3]. BGP-15, a hydroxylamine derivative, is a pharmacological coinducer of Hsp72 (heat shock protein 72), shown safe and well tolerated in phase 2 clinical trials for diabetes and insulin resistance[4]. BGP-15 is also a inhibitor of PARP. BGP-15 either blocked or significantly reduced (60-90% in 100-200 mg/kg oral dose) cisplatin induced increase in serum urea and creatinine level in mice and rats and prevented the structural degeneration of the kidney, as well. The nephroprotective effect of BGP-15 treatment was revealed also in living mice by MRI analysis manifesting in the lack of oedema which otherwise developed as a result of cisplatin treatment. BGP-15 decreased cisplatin-induced ROS production in rat kidney mitochondria and improved the antioxidant status of the kidney in mice with cisplatin-induced nephropathy. In rat kidney, cisplatin caused a decrease in the level of Bcl-x, a mitochondrial protective protein, and this was normalized by BGP-15 treatment. Moreover, treatment with BGP-15 increased the mean survival time of cisplatin-treated P-388 leukemia bearing mice from 13 to 19 days[2].
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
NCT01069965 Diabetes Mellitus Phase 2 Terminated(Funding support wit... 展开 >>hdrawn.) 收起 << - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.28mL

14.23mL

2.85mL

1.42mL

28.47mL

5.69mL

2.85mL
参考文献

[1]Sapra G, Tham YK, et al. The small-molecule BGP-15 protects against heart failure and atrial fibrillation in mice. Nat Commun. 2014 Dec 9;5:5705.

[2]BGP-15 - a novel poly(ADP-ribose) polymerase inhibitor - protects against nephrotoxicity of cisplatin without compromising its antitumor activity

[3]PARP Inhibition in Cancer: An Update on Clinical Development

[4]BGP-15 Improves Aspects of the Dystrophic Pathology in mdx and dko Mice with Differing Efficacies in Heart and Skeletal Muscle