Apabetalone (RVX-08, RVX-000222)

Alias: RVX-000222; RVX208; RVX 000222; RVX 208; RVX000222; RVX-208; Apabetalone.
Cat No.:V0415 Purity: ≥98%
Apabetalone (also known as RVX-208, RVX000222) is a novel and potent inhibitor of BET (Bromodomain and Extra-Terminal) bromodomain (BD) with potential anti-inflammatory activity and the potential to be used in the treatment of cardiovascular diseases.
Apabetalone (RVX-08, RVX-000222) Chemical Structure CAS No.: 1044870-39-4
Product category: Epigenetic Reader Domain
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Purity: ≥98%

Product Description

Apabetalone (also known as RVX-208, RVX000222) is a novel and potent inhibitor of BET (Bromodomain and Extra-Terminal) bromodomain (BD) with potential anti-inflammatory activity and the potential to be used in the treatment of cardiovascular diseases. It inhibits BET (BD2) with an IC50 of 0.510 μM in a cell-free assay, and shows about 170-fold higher selectivity for BD2 over BD1. RVX-208 is currently undergoing phase III clinical trials for reducing the relative risk (RR) of major adverse cardiac events (MACE) in patients with cardiovascular disease (CVD). It acts by binding to the acetyl-lysine binding pocket in a peptide-competitive way. In HepG2 cells, RVX-208 induced messenger ribonucleic acid and protein synthesis of apolipoprotein (apo)A-I.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Apabetalone (RVX-208) competes with binding of an acetylated histone peptide to tandem BD1 BD2 protein constructions of the four BET proteins, exhibiting IC50s between 0.5 and 1.8 µM. Apabetalone promotes the formation of ApoA-I in hepatocytes in vitro, which leads in increased high density lipoprotein cholesterol (HDL-C). Apabetalone predominantly binds to bromodomains of the BET (Bromodomain and Extra Terminal) family, competing for a position bound by the endogenous ligand, acetylated lysine, and that this accounts for its pharmacological effect. increases Apolipoprotein AI (ApoA-I) synthesis through an epigenetic mechanism and shows that BET inhibition may be a promising new approach to the treatment of atherosclerosis. Apabetalone promotes ApoA-I expression in liver cells[2].
ln Vivo
In the study design for the preventive treatment of atherosclerosis, mice are given a Western diet along with 150 mg/kg/dose bid of medication for a duration of 12 weeks. A year after therapy, mice are killed. Both the vehicle treated and the Apabetalone (RVX-208) treated groups show a progressive increase in body weight. After 12 weeks on a Western diet, the Apabetalone treated group's body weight increased by 4 g (from 24 g to 28 g), while the vehicle treated group experienced a 9 g gain (from 25 g to 34 g). The notable reduction in body weight increase observed in mice treated with Apabetalone is not attributable to a decrease in feed intake, indicating a favorable characteristic of the compound. After six and twelve weeks of therapy with either the vehicle or apibetalone, plasma lipid measurements are performed. At six weeks into therapy, mice treated with apibetalone had a considerable rise (~200%) in their HDL-C levels compared to the vehicle control animals. This increase persisted until the 12-week study's conclusion[3].
Animal Protocol
Dissolved in 1N HCl and carboxymethyl cellulose; 60mg/kg; i.v. injection or p.o.
Na ve adult male AGMs
References
[1]. Picaud S, et al. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9.
[2]. McLure KG, et al. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS One. 2013 Dec 31;8(12):e83190.
[3]. Jahagirdar R, et al. A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice. Atherosclerosis. 2014 Sep;236(1):91-100
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H22N2O5
Molecular Weight
370.4
CAS #
1044870-39-4
SMILES
O=C1NC(C2=CC(C)=C(OCCO)C(C)=C2)=NC3=C1C(OC)=CC(OC)=C3
InChi Key
NETXMUIMUZJUTB-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H22N2O5/c1-11-7-13(8-12(2)18(11)27-6-5-23)19-21-15-9-14(25-3)10-16(26-4)17(15)20(24)22-19/h7-10,23H,5-6H2,1-4H3,(H,21,22,24)
Chemical Name
2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one
Synonyms
RVX-000222; RVX208; RVX 000222; RVX 208; RVX000222; RVX-208; Apabetalone.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 74 mg/mL (199.8 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
0.5% CMC Na (1N HCl, PH 2.5-3.0):8 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.6998 mL 13.4989 mL 26.9978 mL
5 mM 0.5400 mL 2.6998 mL 5.3996 mL
10 mM 0.2700 mL 1.3499 mL 2.6998 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Biological Data
  • RVX-208

  • RVX-208
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