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产品描述： BGP-15 is a PARP inhibitor, with an IC50 and a Ki of 120 and 57 μM, respectively. |
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靶点：
PARP:120 μM (IC50);PARP |
体内研究：
BGP-15 (15 mg/kg, p.o.) does not improve skeletal muscle pathology in older mdx mice. In a rat model, 10 days of BGP-15 treatment greatly improves diaphragm muscle fiber function (by about 100%), although it does not reverse diaphragm atrophy. The treatment also provides protection from myosin PTMs associated with HSP72 induction and PARP-1 inhibition, resulting in improvement of mitochondrial function and content. BGP-15 (15 mg/kg per day in saline) treatment has no effect in Ntg mice or an independent cohort of normal adult wild-type mice based on morphology, cardiac function and ECG parameters. Treatment with BGP-15 attenuates the increase in atrial size and lung weight. BGP-15 treatment is able to prevent or reduce episodes of arrhythmia. BGP-15 treatment is associated with a reduced PR interval in the HF+AF model. BGP-15 (10 and 30 mg/kg) increases insulin sensitivity by 50% and 70%, respectively, in cholesterol-fed but not in normal rabbits. After 5 days of treatment with BGP-15, the glucose infusion rate is increased in a dose-dependent manner in genetically insulin-resistant GK rats. The most effective dose is 20 mg/kg, which shows a 71% increase in insulin sensitivity compared to control group |
参考文献：
1. Kennedy TL, et al. BGP-15 Improves Aspects of the Dystrophic Pathology in mdx and dko Mice with Differing Efficacies in Heart and Skeletal Muscle. Am J Pathol. 2016 Dec;186(12):3246-3260 2. Salah H, et al. The chaperone co-inducer BGP-15 alleviates ventilation-induced diaphragm dysfunction. Sci Transl Med. 2016 Aug 3;8(350):350ra10 3. Sapra G, et al. The small-molecule BGP-15 protects against heart failure and atrial fibrillation in mice. Nat Commun. 2014 Dec 9;5:5705 4. Literati-Nagy B, et al. Improvement of insulin sensitivity by a novel drug candidate, BGP-15, in different animal studies. Metab Syndr Relat Disord. 2014 Mar;12(2):125-31 5. Sarszegi Z, et al. BGP-15, a PARP-inhibitor, prevents imatinib-induced cardiotoxicity by activating Akt and suppressing JNK and p38 MAP kinases. Mol Cell Biochem. 2012 Jun;365(1-2):129-37 6. Szabados E, et al. BGP-15, a nicotinic amidoxime derivate protecting heart from ischemia reperfusion injury through modulation of poly(ADP-ribose) polymerase. Biochem Pharmacol. 2000 Apr 15;59(8):937-45. |
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溶解性：
H2O : 100 mg/mL (284.68 mM; Need ultrasonic) DMSO : 11.33 mg/mL (32.25 mM; Need ultrasonic and warming) |
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保存条件：
2-8℃ |
配置溶液浓度参考：
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1mg |
5mg |
10mg |
| 1 mM |
3.593 ml |
17.963 ml |
35.926 ml |
| 5 mM |
0.719 ml |
3.593 ml |
7.185 ml |
| 10 mM |
0.359 ml |
1.796 ml |
3.593 ml |
| 50 mM |
0.072 ml |
0.359 ml |
0.719 ml |
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| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京