Apabetalone (RVX-208)

製品コードS7295 バッチS729505

印刷

化学情報

Chemical Structure Synonyms RVX-000222 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H22N2O5
分子量 370.4 CAS No. 1044870-39-4
Solubility (25°C)* 体外 DMSO 74 mg/mL (199.78 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

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.
in vitro Apabetalone (RVX-208), a BET bromodomain inhibitor, preferentially binds to the second bromodomain found on BET proteins. [1] As a stimulator of apolipoprotein (APO) AI gene expression, it increases apoA-I and HDL-C in vitro. [2] [3]
in vivo Apabetalone (RVX-208) significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways. [3]
特徴 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.

プロトコル(参考用のみ)

キナーゼアッセイ Competitive Histone Displacement Assay (AlphaScreen Assay)
Apabetalone (RVX-208) is tested in experiments run on a PHERAstar FS plate reader using an AlphaScreen 680 excitation/570 emission filter set. IC50 values for this compound are calculated in Prism 5 after normalization against corresponding DMSO controls. Assays are performed according to the manufacturer’s protocol with minor modifications.
動物実験 動物モデル Naïve adult male AGMs
投薬量 ~60 mg/kg
投与方法 Oral gavage or intravenous administration

参考

  • https://pubmed.ncbi.nlm.nih.gov/24248379/
  • https://pubmed.ncbi.nlm.nih.gov/20178050/
  • https://pubmed.ncbi.nlm.nih.gov/20513599/

カスタマーフィードバック

, , BBRC, 2016, 472(4):624-630.

Data from [Data independently produced by , , Sci Rep, 2018, 8(1):11554]

Data from [Data independently produced by , , Acta Pharmacol Sin, 2018, doi:10.1038/s41401-018-0027-5]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The Bromodomain and Extraterminal Protein Inhibitor Apabetalone Ameliorates Kidney Injury in Diabetes by Regulating Cholesterol Accumulation and Modulating the Gut Microbiota [ Kidney Int Rep, 2025, 10(2):522-534] PubMed: 39990894
BET inhibition revealed varying MYC dependency mechanisms independent of gene alterations in aggressive B-cell lymphomas [ Clin Epigenetics, 2024, 16(1):185] PubMed: 39702340
Targeting BRD3 eradicates nuclear TYRO3-induced colorectal cancer metastasis [ Sci Adv, 2023, 9(15):eade3422] PubMed: 37043564
Targeting BRD3 eradicates nuclear TYRO3-induced colorectal cancer metastasis [ Sci Adv, 2023, 9(15):eade3422] PubMed: 37043564
Exploration de la réponse moléculaire à l'inhibition des protéines BET dans les lymphomes B réfractaires [ HAL OPEN SCIENCE, 2023, ] PubMed: None
Breaking boundaries: Pan BETi disrupt 3D chromatin structure, BD2-selective BETi are strictly epigenetic transcriptional regulators [ Biomed Pharmacother, 2022, 152:113230] PubMed: 35687908
Inhibition of BET Family Proteins Suppresses African Swine Fever Virus Infection [ Microbiol Spectr, 2022, 10(4):e0241921] PubMed: 35758684
Selective Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibition by the SCH772984 Compound Attenuates In Vitro and In Vivo Inflammatory Responses and Prolongs Survival in Murine Sepsis Models [ Int J Mol Sci, 2021, 22(19)10204] PubMed: 34638546
Selective Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibition by the SCH772984 Compound Attenuates In Vitro and In Vivo Inflammatory Responses and Prolongs Survival in Murine Sepsis Models [ Int J Mol Sci, 2021, 22(19)10204] PubMed: 34638546
ABCA1 is associated with the development of acquired chemotherapy resistance and predicts poor ovarian cancer outcome [ Cancer Drug Resist, 2021, 4(2):485-502] PubMed: 35582032

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。