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Apabetalone

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Chemical Structure| 1044870-39-4 同义名 : RVX-208;RVX000222
CAS号 : 1044870-39-4
货号 : A161440
分子式 : C20H22N2O5
纯度 : 99%
分子量 : 370.399
MDL号 : MFCD18633270
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(94.49 mM)，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
动物实验配方：
生物活性
靶点

  • BET

    BD2, IC50:0.51 μM
描述 RVX-208 is a derivative of the plant polyphenol resveratrol. It is a domain-selective inhibitor of BETs with 0.51μM and 87μM for BD2 and BD1, respectively. Inhibition of BD2 by RVX-208 only modestly affected BET-dependent gene transcription[3]. RVX-208 at 60μM induced apoA-I mRNA and protein synthesis in HepG2 cells, leading to increased levels of pre-β-migrating and α-lipoprotein particles containing apoA-I (LpA-I) in spent media. Administration of RVX-208 at doses ranging in 15 to 60 mg/kg/day for 63 days increased serum apoA-I and HDL-C levels (60% and 97%, respectively) of african green monkeys. The levels of pre-β1-LpA-I and α1-LpA-I HDL-subparticles were increased as well as adenosine triphosphate binding cassette AI, adenosine triphosphate binding cassette G1, and scavenger receptor class B type I-dependent cholesterol efflux[4].
作用机制 RVX-208 binds to the acetyl-lysine binding pocket in a peptide-competitive manner. It displaces BET proteins from chromatin.[3]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
HepG2 ~60 μM Function assay induces apoA-I mRNA and de novo synthesis of apoA-I. 20513599
U2OS ~5 μM Function assay displaces BET proteins from chromatin 24248379
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
NCT02586155 Diabetes Mellitus, Type 2 ... 展开 >> Coronary Artery Disease Cardiovascular Diseases 收起 << Phase 3 Recruiting October 2018 Israel ... 展开 >> Lady Davis Carmel Medical Center Recruiting Haifa, Israel, 34362 Contact: Basil Lewis, MD 收起 <<
NCT01067820 Coronary Artery Disease Phase 2 Completed - -
NCT00768274 Dyslipidemia ... 展开 >>Atherosclerosis Acute Coronary Syndrome Cardiovascular Disease 收起 << Phase 1 Phase 2 Completed - United States, Texas ... 展开 >> Covance Clinical Research Unit, Inc. Dallas, Texas, United States, 75247 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.70mL

0.54mL

0.27mL

13.50mL

2.70mL

1.35mL

27.00mL

5.40mL

2.70mL
参考文献

[1]Picaud S, Wells C, 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]Bailey D, Jahagirdar R, et al. RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo. J Am Coll Cardiol. 2010 Jun 8;55(23):2580-9.

[3]Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H, Fedorov O, Müller S, Brennan PE, Knapp S, Filippakopoulos P. 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. doi: 10.1073/pnas.1310658110. Epub 2013 Nov 18. PMID: 24248379; PMCID: PMC3856850.

[4]Bailey D, Jahagirdar R, Gordon A, Hafiane A, Campbell S, Chatur S, Wagner GS, Hansen HC, Chiacchia FS, Johansson J, Krimbou L, Wong NC, Genest J. RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo. J Am Coll Cardiol. 2010 Jun 8;55(23):2580-9. doi: 10.1016/j.jacc.2010.02.035. Erratum in: J Am Coll Cardiol. 2010 Aug 31;56(10):825. PMID: 20513599.