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RVX 208 99%

Apabetalone

源叶(MedMol)
S80050
1044870-39-4
C20H22N2O5
370.4
品牌 货号 产品规格 价格(RMB) 库存(上海) 北京 武汉 南京 购买数量
源叶(MedMol) S80050-2mg 99% ¥100.00元 4 - - -
源叶(MedMol) S80050-5mg 99% ¥144.00元 8 - - -
源叶(MedMol) S80050-10mg 99% ¥204.00元 7 - - -
源叶(MedMol) S80050-25mg 99% ¥370.00元 8 - - -
源叶(MedMol) S80050-50mg 99% ¥510.00元 预计交期:2-3天 - - -
源叶(MedMol) S80050-100mg 99% ¥760.00元 4 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87 μM and 0.51 μM for BD1 and BD2, respectively
产品描述: Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87 μM and 0.51 μM for BD1 and BD2, respectively
靶点: IC50: 510±41 nM (BD2), 87±10 μM (BD1);EpigeneticReaderDomain;HIVProtease
体内研究:
In the atherosclerosis prophylactic treatment study design, mice are fed a Western diet concurrent with the treatment with 150 mg/kg/dose b.i.d. for 12 weeks. Mice are sacrificed at 12 weeks after treatment. There is a progressive increase in body weight in both the vehicle treated as well as the Apabetalone (RVX-208) treated groups. However, there is only an increase of 4 g (from 24 g to 28 g) body weight after 12 weeks on Western diet in the Apabetalone treated group whereas this increase is found to be 9 g (25 g-34 g) in the vehicle treated group. The significant decrease in body weight gain in Apabetalone treated mice is not due to decreased feed consumption, suggesting a positive attribute of the molecule. Plasma lipid measurements are done at 6 weeks and 12 weeks of treatment with either the vehicle or Apabetalone. Compared to the vehicle control animals, Apabetalone treated mice show significant increase (~200%) in the levels of HDL-C at 6 weeks of treatment, which is sustained until end of the study (12 weeks)
参考文献:
1. Picaud S, et al. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9. 2. McLure KG, et al. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS One. 2013 Dec 31;8(12):e83190. 3. Jahagirdar R, et al. A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice. Atherosclerosis. 2014 Sep;236(1):91-100.
溶解性: DMSO  :  ≥  33  mg/mL  (89.09  mM)
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.7 ml 13.499 ml 26.998 ml
5 mM 0.54 ml 2.7 ml 5.4 ml
10 mM 0.27 ml 1.35 ml 2.7 ml
50 mM 0.054 ml 0.27 ml 0.54 ml
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参考文献

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