RVX-208 --- BET Bromodomain Inhibitor


Catalog No. size PriceQuantity
M60177-2S 2 mg solid $79
M60177-10S 10 mg solid $316

Description

RVX-208, also known as Apabetalone, is a potent inhibitor of BET bromodomains. RVX-208 functions by removing atherosclerotic plaque via reverse cholesterol transport (RCT). RVX-208 increases the production of ApoA-I in hepatocytes in vitro, and in vivo in monkeys and humans, which results in increased HDL-C, but the molecular target was not previously reported. RVX-208 may be a promising new approach to the treatment of atherosclerosis.

Product information

CAS Number: 1044870-39-4

Molecular Weight: 370.40

Formula: C20H22N2O5

Synonym:

Apabetalone

Chemical Name: 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one

Smiles: CC1C=C(C=C(C)C=1OCCO)C1NC(=O)C2C(=CC(=CC=2N=1)OC)OC

InChiKey: NETXMUIMUZJUTB-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

RVX-208 was used at 10 μM final concentration in various in vitro assays.

In Vivo:

RVX-208 was dosed to naïve adult male African green monkeys (AGMs) by oral gavage or intravenous administration at 60 mg/kg once per day.

References:

  1. Picaud S, Wells C, Felletar I, et al. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A, 2013, 110(49): 19754-19759.
  2. Bailey D, Jahagirdar R, Gordon A, et al. RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo. J Am Coll Cardiol, 2010, 55(23): 2580-2589.
  3. McLure KG, Gesner EM, Tsujikawa L, et al. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS One, 2013, 8(12): e83190.
  4. Jahagirdar R, Zhang H, Azhar S, et al. A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice. Atherosclerosis, 2014, 236(1): 91-100.

Products are for research use only. Not for human use.


Documents

Payment & Security

PayPal Venmo

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed