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Apabetalone

(Synonyms: 阿帕他隆; RVX-208; RVX000222)

目录号: PL13502 纯度: ≥99%

Apabetalone (RVX-208) 是一种 BET 转录抑制剂，作用于 BD1 和 BD2，IC50 分别为 87 μM 和 0.51 μM。

CAS No. :1044870-39-4

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中文名称	Apabetalone
中文别名	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;2-(4-(2-羟基乙氧基)-3,5-二甲基苯基)-5,7-二甲氧基-4(3H)-酮;2-(4-(2-羟基乙氧基)-3,5-二甲基苯基)-5,7-二甲氧基喹唑啉-4(3H)-酮;3-氨基-5-(2-苯基乙基)-1H-吡唑;RVX-208 抑制剂;阿帕他隆
英文名称	Apabetalone
英文别名	RVX-208;RVX 208;2-(4-(2-Hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one;2-(4-(2-Hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquizolin-4(3H)-one;2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-di methoxyquinazolin-4(3H)-one;2-[4-(2-Hydroxy-ethoxy)-3,5-dimethyl-phenyl]-5,7-dimethoxy-3H-quinazolin-4-one;1K0;2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-3H-quinazolin-4-one;Apabetalone;CHEMBL2393130;QC-216;RVX000222;RVX-000222;SureCN145019;UNII-8R4A7GDZ1D;RVX-208(RVX 000222);Apabetalone-RVX-208;4(3H)-Quinazolinone, 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-;2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-4(3H)-quinazolinone RVX-208;2-[4-(2-Hydroxyethoxy)-3,5-Dimethylphenyl]-5,7-Dimethoxyquinazolin-4(3h)-One;RVX 000222;8R4A7GDZ1D;AK110565;Apabetalone [INN];Apabetalone [USAN:INN];4j3i;4mr4;4mr6;4j1p;Apabetalone (USAN/INN);GTPL7034;AOB2133;NETXMUIMUZJUTB-UHFFFAOYSA-N;HMS3744M09;HMS3653C10;RVX-208(RVX000222)
Cas No.	1044870-39-4
分子式	C₂₀H₂₂N₂O₅
分子量	370.40
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Apabetalone (RVX-208) 是一种 BET 转录抑制剂，作用于 BD1 和 BD2，IC₅₀ 分别为 87 μM 和 0.51 μM。

生物活性

Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC 50 s are 87 μM and 0.51 μM for BD1 and BD2, respectively.

性状

Solid

IC50 & Target[1][2]

IC50: 510±41 nM (BD2), 87±10 μM (BD1)

体外研究(In Vitro)

Apabetalone (RVX-208) competes with binding of an acetylated histone peptide to tandem BD1 BD2 protein constructs of the four BET proteins, with IC50s between 0.5 and 1.8 μM. Apabetalone increases the production of ApoA-I in hepatocytes in vitro, which results in increased high density lipoprotein cholesterol (HDL-C). Apabetalone selectively binds to bromodomains of the BET (Bromodomain and Extra Terminal) family, competing for a site bound by the endogenous ligand, acetylated lysine, and that this accounts for its pharmacological activity. Apabetalone increases Apolipoprotein A-I (ApoA-I) production through an epigenetic mechanism and suggests that BET inhibition may be a promising new approach to the treatment of atherosclerosis. Apabetalone increases ApoA-I expression in liver cells. has not independently

体内研究(In Vivo)

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 tre

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : ≥ 33 mg/mL (89.09 mM)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Apabetalone

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