Apabetalone (RVX-208)
别名: RVX-000222 中文名称：阿帕他隆
Apabetalone (RVX-208, RVX-000222) 是一种有效的BET bromodomain抑制剂，作用于BD2， 无细胞试验中IC50为0.510 μM，比作用于BD1选择性高170倍。Phase 2。
Apabetalone (RVX-208) Chemical Structure
CAS: 1044870-39-4
产品质控
批次：
纯度：
99.85%
99.85
Apabetalone (RVX-208)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HepG2 | Function assay | ~60 μM | induces apoA-I mRNA and de novo synthesis of apoA-I. | 20513599 | |
| U2OS | Function assay | ~5 μM | displaces BET proteins from chromatin | 24248379 | |
| MCF7 | Autophagy assay | 150 uM | Induction of autophagy in human MCF7 cells assessed as downregulation of p62/SQSTM1 expression at 150 uM by Western blot analysis | 29172540 | |
| MDA-MB-231 | Autophagy assay | 150 uM | Induction of autophagy in human MDA-MB-231 cells assessed as downregulation of p62/SQSTM1 expression at 150 uM by Western blot analysis | 29172540 | |
| SAE | Function assay | 24 hrs | Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG54 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis, IC50 = 2.63 μM. | 29649741 | |
| SAE | Function assay | 24 hrs | Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG56 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis, IC50 = 2.74 μM. | 29649741 | |
| SAE | Function assay | 24 hrs | Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced grobeta RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis, IC50 = 3.73 μM. | 29649741 | |
| SAE | Function assay | 24 hrs | Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced IL-8 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis, IC50 = 3.85 μM. | 29649741 | |
| MV4-11 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay, IC50 = 4.48 μM. | 28765013 | |
| OCI-AML3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay, IC50 = 7.17 μM. | 28765013 | |
| OCI-AML2 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay, IC50 = 8.31 μM. | 28765013 | |
| BL21(DE3)-R3-pRARE2 | Function assay | Inhibition of recombinant human His6-tagged BRD4 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins followed by HSGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH peptide substrate addition after 30 mins by alphas, Kd = 0.135 μM. | 28195723 | ||
| BL21(DE3) | Function assay | Binding affinity to human BRD4 bromodomain 2 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry, Kd = 0.14 μM. | 26367539 | ||
| BL21(DE3)-R3-pRARE2 | Function assay | Inhibition of recombinant human His6-tagged BRD3 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells, Kd = 0.195 μM. | 28195723 | ||
| BL21(DE3) | Function assay | Binding affinity to human BRD2 bromodomain 2 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry, Kd = 0.25 μM. | 26367539 | ||
| BL21(DE3)-R3-pRARE2 | Function assay | Inhibition of recombinant human His6-tagged BRD2 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells, Kd = 0.251 μM. | 28195723 | ||
| BL21(DE3) | Function assay | Binding affinity to human BRD4 bromodomain 1 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry, Kd = 1.1 μM. | 26367539 | ||
| BL21(DE3)-R3-pRARE2 | Function assay | Inhibition of recombinant human His6-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins followed by H4K5acK8acK12acK16ac peptide substrate addition after 30 mins by alphascreen assay, Kd = 1.142 μM. | 28195723 | ||
| BL21(DE3)-R3-pRARE2 | Function assay | Inhibition of recombinant human His6-tagged BRD3 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells, Kd = 4.065 μM. | 28195723 | ||
| BL21(DE3)-R3-pRARE2 | Function assay | Inhibition of recombinant human His6-tagged BRD2 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells, Kd = 5.78 μM. | 28195723 | ||
| BL21(DE3) | Function assay | Binding affinity to human BRD2 bromodomain 1 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry, Kd = 5.8 μM. | 26367539 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Apabetalone (RVX-208, RVX-000222) 是一种有效的BET bromodomain抑制剂，作用于BD2， 无细胞试验中IC50为0.510 μM，比作用于BD1选择性高170倍。Phase 2。 | ||
|---|---|---|---|
| 特性 | 首创新药BD2选择性BET溴结构域蛋白抑制剂在II期临床试验中进行测试，用于冠状动脉综合症和动脉粥样硬化的治疗。 | ||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 作为BET溴结构域蛋白抑制剂，RVX-208优先与基于BET蛋白质的第二溴结构域蛋白结合。[1] RVX-208，作为载脂蛋白(APO) AI基因表达的激动剂，在体外增加apoA-I 和 HDL-C。[2] [3] | |||
|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p21 / p24 / β-actin cyclin D1 / CDK4 / CDK6 / p24 / β-actin Rb / p-Rb(S780) / p-Rb(S795) / p-Rb(S807/811) / β-actin Cyclin T1 / CDK9-55kDa / CDK9-42kDa / p-CDK9 / CTD / CTD-Ser2P / p24 / β-actin Phospho-RelA / Total-RelA / Actin / BRD2 / α-Tubulin |
|
29789664 | |
| Immunofluorescence | monocyte adhesion DNA SARS-CoV-2 CTNT |
|
31300040 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | RVX-208显著增加AGMs中血清apoA-I和 HDL-C，并通过不同途径增加胆固醇流出。[3] | |
|---|---|---|
| 动物实验 | Animal Models | 天然成年雄性 AGMs |
| Dosages | ~60 毫克/千克 | |
| Administration | 口服灌胃或静脉注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03160430 | Not yet recruiting | Kidney Failure Chronic |
Resverlogix Corp |
November 22 2024 | Phase 1|Phase 2 |
| NCT03228940 | Withdrawn | Fabry Disease |
Resverlogix Corp |
November 22 2022 | Phase 1|Phase 2 |
| NCT01863225 | Terminated | Dyslipidemia|Coronary Artery Disease |
Resverlogix Corp|South Australian Health and Medical Research Institute |
May 2013 | Phase 2 |
| NCT01728467 | Completed | Diabetes |
Resverlogix Corp|Baker Heart and Diabetes Institute|Nucleus Network Ltd |
November 2012 | Phase 2 |
| NCT01067820 | Completed | Coronary Artery Disease |
Resverlogix Corp|The Cleveland Clinic |
September 2011 | Phase 2 |
| NCT01423188 | Completed | Coronary Artery Disease|Dyslipidemia |
Resverlogix Corp|The Cleveland Clinic |
August 2011 | Phase 2 |
化学信息&溶解度
| 分子量 | 370.4 | 分子式 | C20H22N2O5 |
| CAS号 | 1044870-39-4 | SDF | Download Apabetalone (RVX-208) SDF |
| Smiles | CC1=CC(=CC(=C1OCCO)C)C2=NC3=C(C(=CC(=C3)OC)OC)C(=O)N2 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 74 mg/mL ( (199.78 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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