Apabetalone

SKU: orb1305422

Description

Apabetalone (RVX-000222) is a selective BET bromodomain inhibitor investigated for cardiovascular and metabolic diseases. Research demonstrates its potential in preclinical models of atherosclerosis and diabetes, showing modulation of key inflammatory and fibrotic pathways in both in vitro and in vivo studies.

Research Area

Epigenetics & Chromatin, Infectious Disease & Virology, Protein Biochemistry

Key Properties

• CAS Number: 1044870-39-4
• MW: 370.4
• Purity: >99.99% (May vary between batches)
• Formula: C₂₀H₂₂N₂O₅
• SMILES: COc1cc(OC)c2c(c1)[nH]c(nc2=O)-c1cc(C)c(OCCO)c(C)c1
• Target: Epigenetic Reader Domain,HIV Protease
• Solubility: DMSO:60 mg/mL (161.99 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.4 mM)

Bioactivity

• Target IC50:
  BD2:0.51 μM
• In Vivo:
  In vitro studies have demonstrated that RVX-208 activates the expression of the apolipoprotein AI gene, leading to an increase in apoA-I and HDL-C levels. Additionally, RVX-208 inhibits BET bromodomain proteins, exhibiting a preferential binding to the second bromodomain of BET proteins.
• In Vitro:
  In AGMs, RVX-208 significantly increases serum apoA-I and HDL-C levels and enhances cholesterol efflux through various pathways.
• Cell Research:
  RVX-208 is prepared in DMSO and stored, and then diluted with appropriate medium before use. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RVX 000222, RVX 208, RVX000222, RVX-000222, RVX208, RVX-208, BD2, Apabetalone, EpigeneticReaderDomain, Epigenetic Reader Domain, HIVProtease, HIV, HIV Protease, Human immunodeficiency virus, inhibit, Inhibitor

Compound Identifiers

PubChem CID

135564749