Welcome to LookChem.com Sign In|Join Free

CAS

  • or

1044870-39-4

Post Buying Request

1044870-39-4 Suppliers

Recommended suppliersmore

  • Product
  • FOB Price
  • Min.Order
  • Supply Ability
  • Supplier
  • Contact Supplier

1044870-39-4 Usage

Description

The bromodomain and extra terminal (BET) proteins interact with acetylated lysine-containing sequences on target proteins via their bromodomains, commonly altering gene transcription. The human BET proteins contain two bromodomains, the first (BD1) being closer to the N-terminus than the second (BD2). RVX-208 is a selective antagonist of BET bromodomains, binding with 10-100-fold higher affinity for BD2 (IC50 = 0.04-0.28 μM) over BD1 (IC50 = 1.8-3.1 μM). RVX-208 causes the selective release of BET proteins from chromatin in cells. It interferes with the BET protein BRD4, resulting in an increased expression of apolipoprotein (Apo) A1 in cells, mice, monkeys, and humans. RVX-208 also reduces atherosclerosis in hyperlipidemic ApoE-deficient mice.

Uses

RVX-208 is a selective antagonist of bromodomain and extra terminal (BET)’s bromodomains.

References

1) Picaud?et al. (2013),?RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain; Proc. Natl. Acad. Sci. USA,?110?19754 2) McLure?et al. (2013),?RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist; PLoS One,?8e83190 3) Bailey?et al. (2010),?RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo; J. Am. Coll. Cardiol.,?55?2580 4) Jahagirdar?et al. (2014),?A novel BET bromodomain inhibitor, RVX-208 shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice; Atherosclerosis,?236?91

Check Digit Verification of cas no

The CAS Registry Mumber 1044870-39-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,4,4,8,7 and 0 respectively; the second part has 2 digits, 3 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 1044870-39:
(9*1)+(8*0)+(7*4)+(6*4)+(5*8)+(4*7)+(3*0)+(2*3)+(1*9)=144
144 % 10 = 4
So 1044870-39-4 is a valid CAS Registry Number.

1044870-39-4SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 19, 2017

Revision Date: Aug 19, 2017

1.Identification

1.1 GHS Product identifier

Product name 2-(4-(2-Hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one

1.2 Other means of identification

Product number -
Other names 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-1H-quinazolin-4-one

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:1044870-39-4 SDS

1044870-39-4Downstream Products

1044870-39-4Relevant articles and documents

Method for preparing apabetalone, intermediates and preparation method of intermediates

-

Paragraph 0085-0092, (2020/05/30)

The invention provides a preparation method of apabetalone. The preparation method comprises the step of reacting a first intermediate, namely 2-bromo-4,6-dimethoxybenzoic acid with a second intermediate, namely 4-(2-hydroxyethoxy)-3,5-dimethylbenzamidine hydrochloride in an alkali-containing organic solvent under the action of a catalyst so as to obtain apabetalone. According to the invention, total yield is 33.4% or above, raw materials are easy to obtain, process is simple, reaction conditions are mild, post-treatment method is simple, the yield of each step and the total yield are high, and cost can be reduced. Apabetalone is a medicine for treating cardiovascular diseases such as atherosclerosis and the like, and has good application prospects. The invention also provides the intermediate 4-(2-hydroxyethoxy)-3,5-dimethylbenzamidine hydrochloride for synthesizing apabetalone and a preparation method thereof, and a preparation method of the compound 2-bromo-4,6-dimethoxybenzoic acid.

Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208

Yu, Ping,Liu, Wenjing,Ren, Jinghui,Wang, Yingying,Ning, Yao,Huang, Mingqi,Hu,Wei, Lili,Ji, Min,Cai, Jin

, p. 2168 - 2172 (2019/07/03)

Bromodomain-containing protein 4 (BRD4) is a new therapeutic target for the treatment of diseases including cardiovascular diseases, cancer, inflammation and central nervous system (CNS) disorders. In this study, we introduced the pharmacophore of fibrates to a BRD4 inhibitor, RVX-208, to design dual-active hypolipidemic compounds, and found that some of new analogues showed favorable hypolipidemic activities. Synthetic accessibility towards this class of compounds optimized RVX-208 as well as would supply more thoughts on hypolipidemic drugs.

Preparation method for Apabetalone

-

, (2018/07/30)

The invention relates to a preparation method for Apabetalone, and particularly discloses a synthesis method for Apabetalone. The preparation method comprises the following steps: (1) a first intermediate, i.e., 2-bromo-4,6-dimethoxy benzamide, is prepared; (2) a second intermediate, i.e., 4-{2-[(t-butyldimethylsilicon)oxy]ethyoxyl}-3,5-dimethyl benzaldehyde, is prepared; (3) the first intermediate and the second intermediate are sealed under the conditions of cuprous bromide, cesium carbonate, L-proline and ammonia hydroxide to react, so that Apabetalone is obtained. The preparation method disclosed by the invention is simple, and yield is high.

Post a RFQ

Enter 15 to 2000 letters.Word count: 0 letters

Attach files(File Format: Jpeg, Jpg, Gif, Png, PDF, PPT, Zip, Rar,Word or Excel Maximum File Size: 3MB)

1

What can I do for you?
Get Best Price

Get Best Price for 1044870-39-4