Apabetalone (RVX-208)

別名:RVX-000222

Apabetalone (RVX-208, RVX-000222) is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2.

Apabetalone (RVX-208)化学構造

CAS No. 1044870-39-4

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 40500 国内在庫あり
JPY 133500 国内在庫あり
JPY 190500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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現在のバッチを見る: 純度: 99.85%
99.85

Apabetalone (RVX-208)関連製品

Epigenetic Reader Domain阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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
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生物活性

製品説明 Apabetalone (RVX-208, RVX-000222) is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2.
特性 First-in-class BD2-selective inhibitor of BET bromodomain and has been tested in Phase II clinical trials for treatment of coronary syndromes and atherosclerosis.
Targets
BD2 [1]
(Cell-free assay)
0.51 μM
In Vitro
In vitro As a BET bromodomain inhibitor, RVX-208 preferentially binds to the second bromodomain found on BET proteins. [1] RVX-208, as a stimulator of apolipoprotein (APO) AI gene expression, increases apoA-I and HDL-C in vitro. [2] [3]
実験結果図 Methods Biomarkers 結果図 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
In Vivo
In Vivo RVX-208 significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways. [3]
動物実験 動物モデル Naïve adult male AGMs
投与量 ~60 mg/kg
投与経路 Oral gavage or intravenous administration
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

化学情報

分子量 370.4 化学式

C20H22N2O5

CAS No. 1044870-39-4 SDF Download Apabetalone (RVX-208) SDFをダウンロードする
Smiles CC1=CC(=CC(=C1OCCO)C)C2=NC3=C(C(=CC(=C3)OC)OC)C(=O)N2
保管

In vitro
Batch:

DMSO : 74 mg/mL ( (199.78 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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