Free shipping on all orders over $ 500

RVX-208

Cat. No. M2219
RVX-208 Structure
Synonym:

RVX000222; Apabetalone

Size Price Availability Quantity
10mM*1mL in DMSO USD 39  USD39 In stock
5mg USD 36  USD36 In stock
10mg USD 53  USD53 In stock
50mg USD 135  USD135 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Apabetalone (RVX-208) is a first-in-class, small molecule that inhibits BET bromodomains. RVX-208 binds to the BET protein, it triggers a cascade of events leading to increased ApoA-I gene transcription and eventually production of the protein. RVX-208 increases apoA-I and HDL-C in vitro and in vivo. In AGMs, RVX-208 raises serum pre-beta(1)-LpA-I and alpha-LpA-I levels and enhances cholesterol efflux.

Chemical Information
Molecular Weight 370.4
Formula C20H22N2O5
CAS Number 1044870-39-4
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Gopal C Ghosh, et al. RVX 208: A novel BET protein inhibitor, role as an inducer of apo A-I/HDL and beyond

[2] Dragana Nikolic, et al. An evaluation of RVX-208 for the treatment of atherosclerosis

[3] Kevin G McLure, et al. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist

[4] No authors listed. Drugs R D. Rvx 208

[5] Eileen McNeill. RVX-208, a stimulator of apolipoprotein AI gene expression for the treatment of cardiovascular diseases

Related Epigenetic Reader Domain Products
Phoenixin-20

Phoenixin-20 (PNX-20) is a bioactive peptide with hormone-like actions in vertebrates, and can stimulates hypothalamo-pituitary-gonadal hormones and regulate reproductive processes in mammals.

Menin-MLL inhibitor 31

Menin-MLL inhibitor 31 is a potent inhibitor of the menin MLL interaction with an IC50 value of 4.6 nM.

OPN-2853

OPN-2853 is a bromodomain protein-4 (BRD4) inhibitor that can be used in studies related to hematologic and lymphatic disorders.

HDAC/JAK/BRD4-IN-1

HDAC/JAK/BRD4-IN-1 is a potent HDAC/JAK/BRD4 triple inhibitor.

VYN-201

VYN-201 is a novel pan-BET inhibitor for studies related to idiopathic pulmonary fibrosis.

  Catalog
Abmole Inhibitor Catalog




Keywords: RVX-208, RVX000222; Apabetalone supplier, Epigenetic Reader Domain, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.