源叶(MedMol)
S80050
一键复制产品信息
1044870-39-4
C20H22N2O5
370.4
2-[3,5-二甲基-4-(2-羟基乙氧基)苯基]-5,7-二甲氧基喹唑啉-4(3H)-酮
RVX 208 99.96%
| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S80050-2mg |
99.96% | ￥100.00 |
7 | - | - | - | - |
|
S80050-5mg |
99.96% | ￥120.00 |
8 | - | - | - | - |
|
S80050-10mg |
99.96% | ￥184.00 |
10 | - | - | - | - |
|
S80050-25mg |
99.96% | ￥268.00 |
8 | - | - | - | - |
|
S80050-50mg |
99.96% | ￥460.00 |
1 | - | - | - | - |
|
S80050-100mg |
99.96% | ￥680.00 |
3 | - | - | - | - |
|
| 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： |
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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。 |
参考文献
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