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S80878

BGP-15

源叶(MedMol) 98%
  • 英文名:
  • (Z)-N'-(2-hydroxy-3-(piperidin-1-yl)propoxy)nicotiniMidaMide
  • 别名:
  • (Z)-N'-(2-Hydroxy-3-(piperidin-1-yl)propoxy)nicotiniMidaMide dihydrochloride;N-(2-Hydroxy-3-(piperidin-1-yl)propoxy)-nicotinimidamide dihy
  • CAS号:
  • 66611-37-8
  • 分子式:
  • C14H22N4O2
  • 分子量:
  • 278.35008
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S80878-1mg 98% ¥106.00元 10 - - - EA 加入购物车
源叶(MedMol) S80878-5mg 98% ¥315.00元 6 - - - EA 加入购物车
源叶(MedMol) S80878-10mg 98% ¥590.00元 6 - - - EA 加入购物车
源叶(MedMol) S80878-25mg 98% ¥1290.00元 6 - - - EA 加入购物车
源叶(MedMol) S80878-50mg 98% ¥1930.00元 5 - - - EA 加入购物车
源叶(MedMol) S80878-100mg 98% ¥2650.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: BGP-15 is a PARP inhibitor, with an IC50 and a Ki of 120 and 57 μM, respectively.
  • 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.
  • 溶解性: H2O  :  100  mg/mL  (284.68  mM;  Need  ultrasonic)    DMSO  :  11.33  mg/mL  (32.25  mM;  Need  ultrasonic  and  warming)
  • 保存条件: 2-8℃
  • 配置溶液浓度参考:
    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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