Apabetalone (Synonyms: 阿帕他隆; RVX-208; RVX000222)

目录号: HY-16652 纯度: 99.47%: FAQs
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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。

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Apabetalone Chemical Structure

CAS No. : 1044870-39-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥550	In-stock
1 mg	￥250	In-stock
5 mg	￥500	In-stock
10 mg	￥830	In-stock
25 mg	￥1438	In-stock
50 mg	￥2088	In-stock
100 mg	￥3225	In-stock
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500 mg		询价

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Customer Review

MCE 顾客使用本产品发表的 6 篇科研文献

: Apabetalone purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2016 Dec;1859(12):1527-1537. [Abstract]; RVX208 increases CTGF and CYR61 expression and TAZ protein level in HCT116 cells.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

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^[1].

IC₅₀ & Target

IC50: 510±41 nM (BD2), 87±10 μM (BD1)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
697	EC₅₀	> 5 μM Compound: 3; RVX-208	Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 29170024]
A-375	IC₅₀	240.9 μM Compound: RVX-208	Antiproliferative activity against human A375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human A375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
A549	IC₅₀	53.1 μM Compound: RVX-208	Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
CCRF-CEM	EC₅₀	> 5 μM Compound: RVX-028	Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability incubated for 72 hrs Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability incubated for 72 hrs	[PMID: 35348328]
DLD-1	IC₅₀	> 10 μM Compound: RVX-208	Antiproliferative activity against human DLD1 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay Antiproliferative activity against human DLD1 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay	[PMID: 32153186]
HCT-116	IC₅₀	12.83 μM Compound: RVX-208	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay	[PMID: 32153186]
HepG2	IC₅₀	103 μM Compound: RVX-208	Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
HL-60	IC₅₀	> 20 μM Compound: 2; RVX-208	Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 24 hrs by MTT assay Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 24 hrs by MTT assay	[PMID: 27266999]
HT-29	IC₅₀	235.8 μM Compound: RVX-208	Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
K562	EC₅₀	> 5 μM Compound: RVX-028	Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs	[PMID: 35348328]
L02	IC₅₀	> 100 μM Compound: RVX-208	Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 24 hrs by MTT assay Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 24 hrs by MTT assay	[PMID: 30926312]
LOUCY	EC₅₀	> 5 μM Compound: 3; RVX-208	Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 29170024]
MCF7	IC₅₀	> 300 μM Compound: RVX-208	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
MCF7	IC₅₀	140.1 μM Compound: 2a; RVX-208	Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay	[PMID: 29172540]
MDA-MB-231	IC₅₀	155.4 μM Compound: 2a; RVX-208	Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay	[PMID: 29172540]
MOLM-14	EC₅₀	6.7 μM Compound: RVX-028	Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs	[PMID: 35348328]
MV4-11	IC₅₀	> 20 μM Compound: 2; RVX-208	Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 24 hrs by MTT assay Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 24 hrs by MTT assay	[PMID: 27266999]
MV4-11	IC₅₀	4.48 μM Compound: 1; RVX-208	Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay	[PMID: 28765013]
NALM-6	EC₅₀	> 5 μM Compound: 3; RVX-208	Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 29170024]
NB-4	EC₅₀	> 5 μM Compound: RVX-028	Cytotoxicity against human NB-4 cells assessed as reduction in cell viability incubated for 72 hrs Cytotoxicity against human NB-4 cells assessed as reduction in cell viability incubated for 72 hrs	[PMID: 35348328]
NRK-49F	IC₅₀	42 μM Compound: RVX-208	Antifibrotic activity against rat NRK-49F cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antifibrotic activity against rat NRK-49F cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
OCI-AML2	IC₅₀	8.31 μM Compound: 1; RVX-208	Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay	[PMID: 28765013]
OCI-AML-3	IC₅₀	7.17 μM Compound: 1; RVX-208	Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay	[PMID: 28765013]
SW-620	IC₅₀	> 10 μM Compound: RVX-208	Antiproliferative activity against human SW620 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay Antiproliferative activity against human SW620 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay	[PMID: 32153186]
U-937	IC₅₀	> 20 μM Compound: 2; RVX-208	Cytotoxicity against human U937 cells assessed as decrease in cell viability after 24 hrs by MTT assay Cytotoxicity against human U937 cells assessed as decrease in cell viability after 24 hrs by MTT assay	[PMID: 27266999]

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^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 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)^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

370.40

Formula

C₂₀H₂₂N₂O₅

CAS 号

1044870-39-4

性状

固体

颜色

White to yellow

中文名称

阿帕他隆

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
In solvent	-80°C	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 33 mg/mL (89.09 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6998 mL	13.4989 mL	26.9978 mL
5 mM	0.5400 mL	2.6998 mL	5.3996 mL
10 mM	0.2700 mL	1.3499 mL	2.6998 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.75 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.75 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.75 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
方案四

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (6.75 mM); 澄清溶液
方案五

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.75 mM); 澄清溶液
方案六

请依序添加每种溶剂： 1% DMSO 99% Saline
Solubility: ≥ 0.5 mg/mL (1.35 mM); 澄清溶液

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 50% PEG300 50% Saline
Solubility: 15.15 mg/mL (40.90 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.47%

选择批次：

Data Sheet (627 KB) SDS (393 KB)

COA (190 KB) LCMS (267 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Cell Assay ^[2]	Huh7 cells are plated at 23,000/well in a 96 well plate in DMEM+10% FBS before allowing to grow overnight. Cells are treated with compounds for 48 h in 0.1% DMSO with or without 5 µM Actinomycin D. U937 cells are differentiated for 3 days in 60 ng/mL PMA, 32,000 cells/well in 96-well format. Cells are then treated with compound in 0.1% DMSO in RPMI media+10% FBS, and after 1 h, lipopolysaccharide is added to the cells at 1 µg/mL for 3 hours^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Mice^[3] Seven to eight week old male ApoE^-/- mice are used. Based on the body weight and lipid values, mice are divided into 2 groups (n=12): group 1, vehicle; and group 2, test agent, Apabetalone. Mice are then switched to Western diet (0.15% cholesterol and 42% calories from fat) and concurrently treated orally by gavage with either vehicle or the test agent, Apabetalone (150 mg/kg/dose b.i.d) for 12 weeks. After 6 week of treatment, an interim blood draw is done to monitor serum lipid levels. After 12 weeks of treatment mice are sacrificed to measure blood lipid parameters, aortic lesion, and liver and aortic RNA. Eight mice are used for enface (aortic plaque) analysis, 4 mice for tissue collection for mRNA and all 12 mice used for aortic sinus lesion area measurement. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief] [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. [Content Brief] [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. [Content Brief]

Apabetalone 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6998 mL	13.4989 mL	26.9978 mL	67.4946 mL
	5 mM	0.5400 mL	2.6998 mL	5.3996 mL	13.4989 mL
	10 mM	0.2700 mL	1.3499 mL	2.6998 mL	6.7495 mL
	15 mM	0.1800 mL	0.8999 mL	1.7999 mL	4.4996 mL
	20 mM	0.1350 mL	0.6749 mL	1.3499 mL	3.3747 mL
	25 mM	0.1080 mL	0.5400 mL	1.0799 mL	2.6998 mL
	30 mM	0.0900 mL	0.4500 mL	0.8999 mL	2.2498 mL
	40 mM	0.0675 mL	0.3375 mL	0.6749 mL	1.6874 mL
	50 mM	0.0540 mL	0.2700 mL	0.5400 mL	1.3499 mL
	60 mM	0.0450 mL	0.2250 mL	0.4500 mL	1.1249 mL
	80 mM	0.0337 mL	0.1687 mL	0.3375 mL	0.8437 mL

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Apabetalone1044870-39-4RVX-208 RVX000222阿帕他隆RVX208RVX 208RVX000222RVX 000222RVX-000222Epigenetic Reader DomainHIVHuman immunodeficiency virusInhibitorinhibitorinhibit

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Apabetalone (Synonyms: 阿帕他隆; RVX-208; RVX000222)

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MCE 顾客使用本产品发表的 6 篇科研文献

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Apabetalone (Synonyms: 阿帕他隆; RVX-208; RVX000222)

Customer Review

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MCE 顾客使用本产品发表的 6 篇科研文献

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F

G

H

J

L

N

Q

S

T

X

Y

Z