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Apabetalone (RVX-208)
別名: RVX-000222 中文名稱：阿帕他隆
Apabetalone (RVX-208, RVX-000222) 是一種有效的BET bromodomain抑制劑，作用于BD2， 無細胞試驗中IC50為0.510 μM，比作用于BD1選擇性高170倍。Phase 2。
Apabetalone (RVX-208) Chemical Structure
CAS: 1044870-39-4
產品質控
批次：
純度：
99.85%
99.85
Apabetalone (RVX-208)相關產品
相關信號通路圖
細胞實驗數據示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數據 | |||||
生物活性
| 產品描述 | Apabetalone (RVX-208, RVX-000222) 是一種有效的BET bromodomain抑制劑，作用于BD2， 無細胞試驗中IC50為0.510 μM，比作用于BD1選擇性高170倍。Phase 2。 | ||
|---|---|---|---|
| 特性 | 首創(chuàng)新藥BD2選擇性BET溴結構域蛋白抑制劑在II期臨床試驗中進行測試，用于冠狀動脈綜合癥和動脈粥樣硬化的治療。 | ||
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | 作為BET溴結構域蛋白抑制劑，RVX-208優(yōu)先與基于BET蛋白質的第二溴結構域蛋白結合。[1] RVX-208，作為載脂蛋白(APO) AI基因表達的激動劑，在體外增加apoA-I 和 HDL-C。[2] [3] | |||
|---|---|---|---|---|
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | 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 | |
| 體內研究(In Vivo) | ||
| 體內研究活性 | RVX-208顯著增加AGMs中血清apoA-I和 HDL-C，并通過不同途徑增加膽固醇流出。[3] | |
|---|---|---|
| 動物實驗 | Animal Models | 天然成年雄性 AGMs |
| Dosages | ~60 毫克/千克 | |
| Administration | 口服灌胃或靜脈注射 | |
| 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 |
化學信息&溶解度
| 分子量 | 370.4 | 分子式 | C20H22N2O5 |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 74 mg/mL ( (199.78 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內配方計算器 | ||||
實驗計算
動物體內配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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