RVX-208

Product Name: RVX-208
CAS No.: 1044870-39-4
Chemical Name: RVX-208
Synonyms: CS-686;CS-1815;RVX-208;RVX-000222;Apabetalone;RVX-208 USP/EP/BP;RVX-208(RVX000222);RVX-208(RVX 000222);Apabetalone-RVX-208;Apabetalone, 10 mM in DMSO
CBNumber: CB52640278
Molecular Formula: C20H22N2O5
Formula Weight: 370.4
MOL File: 1044870-39-4.mol

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RVX-208 Property

Boiling point:: 594.2±60.0 °C(Predicted)
Density: 1.28±0.1 g/cm3(Predicted)
storage temp.: -20°C (des.)
solubility: Soluble in DMSO (up to 75 mg/ml) or in Ethanol (up to 4 mg/ml).
form: solid
pka: 14.21±0.10(Predicted)
color: White
Stability:: Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H371May cause damage to organs

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P309+P311IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 16424
Product name: RVX-208
Purity: ≥98%
Packaging: 1mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 16424
Product name: RVX-208
Purity: ≥98%
Packaging: 5mg
Price: $109
Updated: 2024/03/01

Cayman Chemical

Product number: 16424
Product name: RVX-208
Purity: ≥98%
Packaging: 10mg
Price: $193
Updated: 2024/03/01

Cayman Chemical

Product number: 16424
Product name: RVX-208
Purity: ≥98%
Packaging: 25mg
Price: $404
Updated: 2024/03/01

TRC

Product number: R800000
Product name: RVX208
Packaging: 25mg
Price: $330
Updated: 2021/12/16

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RVX-208 Chemical Properties,Usage,Production

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.

in vivo

In the atherosclerosis prophylactic treatment study design, mice are fed a Western diet concurrent with the treatment with 150 mg/kg/dose b.i.d. for 12 weeks. Mice are sacrificed at 12 weeks after treatment. There is a progressive increase in body weight in both the vehicle treated as well as the Apabetalone (RVX-208) treated groups. However, there is only an increase of 4 g (from 24 g to 28 g) body weight after 12 weeks on Western diet in the Apabetalone treated group whereas this increase is found to be 9 g (25 g-34 g) in the vehicle treated group. The significant decrease in body weight gain in Apabetalone treated mice is not due to decreased feed consumption, suggesting a positive attribute of the molecule. Plasma lipid measurements are done at 6 weeks and 12 weeks of treatment with either the vehicle or Apabetalone. Compared to the vehicle control animals, Apabetalone treated mice show significant increase (~200%) in the levels of HDL-C at 6 weeks of treatment, which is sustained until end of the study (12 weeks)^[3].

target

BD2

References

[1] SARAH PICAUD. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2013, 110 49: 19754-19759. DOI:10.1073/pnas.1310658110
[2] KEVIN G MCLURE. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.[J]. PLoS ONE, 2013: e83190. DOI:10.1371/journal.pone.0083190
[3] RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo
[4] RAVI JAHAGIRDAR . A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice[J]. Atherosclerosis, 2014, 236 1: Pages 91-100. DOI:10.1016/j.atherosclerosis.2014.06.008

RVX-208 Preparation Products And Raw materials

Raw materials

Preparation Products

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RVX-208 Suppliers

China 181 India 3 The Netherlands 1 United Kingdom 1 United States 17 Global 203

Shanghai Boyle Chemical Co., Ltd.

Tel
Fax: 86-21-57758967
Email: sales@boylechem.com
Country: China
ProdList: 2922
Advantage: 55

Chembest Research Laboratories Limited

Tel: +86-21-20908456
Fax: 021-58180499
Email: sales@BioChemBest.com
Country: China
ProdList: 6003
Advantage: 61

Nanjing Chemlin Chemical Co., Ltd

Tel: 025-83697070
Fax: +86-25-83453306
Email: info@chemlin.com.cn
Country: China
ProdList: 15883
Advantage: 64

Dalian Meilun Biotech Co., Ltd.

Tel: 0411-62910999 13889544652
Email: sales@meilune.com
Country: China
ProdList: 4747
Advantage: 58

ShangHai YuanYe Biotechnology Co., Ltd.

Tel: 021-61312847 13636370518
Fax: 021-55068248
Email: shyysw007@163.com
Country: China
ProdList: 4999
Advantage: 60

NCE Biomedical Co.,Ltd.

Tel: 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax: +86-27-87599188
Country: China
ProdList: 1493
Advantage: 55

Shanghai Famo Bio-chemical Technology Company Ltd.

Tel: 021-02136680027 15800370750
Email: 1706640024@qq.com
Country: China
ProdList: 570
Advantage: 56

Haoyuan Chemexpress Co., Ltd.

Tel: 021-58950125
Fax: (86) 21-58955996
Email: info@chemexpress.com
Country: China
ProdList: 7552
Advantage: 61

MedChemexpress LLC

Tel: 021-58955995
Fax: 609-228-5909
Email: sales@medchemexpress.cn
Country: United States
ProdList: 4861
Advantage: 58

Guangzhou Isun Pharmaceutical Co., Ltd

Tel: 020-39119399 18927568969
Fax: 020-39119999
Email: isunpharm@qq.com
Country: China
ProdList: 4720
Advantage: 55

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View Lastest Price from RVX-208 manufacturers

Career Henan Chemical Co

Product: RVX-208 1044870-39-4
Price: US $1.00/g
Min. Order: 100g
Purity: 99%
Supply Ability: G/KG/T
Release date: 2019-12-20

1044870-39-4, RVX-208Related Search:

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2-(4-(2-hydroxyethoxy)-3,5-diMethylphenyl)-5,7-diMethoxyquinazolin-4(3H)-one

RVX-000222

4(3H)-Quinazolinone, 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-

2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-4(3H)-quinazolinone RVX-208

RVX-208

Apabetalone

Apabetalone-RVX-208

RVX-208(RVX 000222)

RVX-208(RVX000222)

CS-1815

APABETALONE; RVX-000222; RVX208; RVX 208; RVX000222; RVX 000222

CS-686

RVX-208 USP/EP/BP

Apabetalone (RVX-08, RVX-000222)

Apabetalone (RVX-208, RVX-000222)

2-(4-(2-Hydroxyethoxy)-2,6-dimethylphenyl)-6,8-dimethoxyquinazolin-4(3H)-one

2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-4aH-quinazolin-4-one

Apabetalone, 10 mM in DMSO

2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-1,4-dihydroquinazolin-4-one

1044870-39-4

Inhibitors

API