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CAS No.: 1044870-39-4

阿帕他隆 Catalog No. CSN13057

Synonyms: RVX-208;RVX000222;阿帕他隆

RVX-208 is an inhibitor of BET bromodomain BD2 with IC50 of 0.510 μM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Bromodomain 2

IC50:0.510μM
描述RVX-208 is a derivative of the plant polyphenol resveratrol. It is a domain-selective inhibitor of BETs with 0.51μM and 87μM for BD2 and BD1, respectively. Inhibition of BD2 by RVX-208 only modestly affected BET-dependent gene transcription^[3]. RVX-208 at 60μM induced apoA-I mRNA and protein synthesis in HepG2 cells, leading to increased levels of pre-β-migrating and α-lipoprotein particles containing apoA-I (LpA-I) in spent media. Administration of RVX-208 at doses ranging in 15 to 60 mg/kg/day for 63 days increased serum apoA-I and HDL-C levels (60% and 97%, respectively) of african green monkeys. The levels of pre-β1-LpA-I and α1-LpA-I HDL-subparticles were increased as well as adenosine triphosphate binding cassette AI, adenosine triphosphate binding cassette G1, and scavenger receptor class B type I-dependent cholesterol efflux^[4].
作用机制RVX-208 binds to the acetyl-lysine binding pocket in a peptide-competitive manner. It displaces BET proteins from chromatin.^[3]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HepG2	~60 μM	Function assay	-	induces apoA-I mRNA and de novo synthesis of apoA-I.	20513599
U2OS	~5 μM	Function assay	-	displaces BET proteins from chromatin	24248379

动物研究
剂量
Mice: 150 mg/kg^[3] (p.o., BID) African green monkey：7.5 mg/kg - 30 mg/kg^[4] (p.o., BID)

给药途径
p.o.
临床研究

动物研究
剂量	Mice: 150 mg/kg^[3] (p.o., BID) African green monkey：7.5 mg/kg - 30 mg/kg^[4] (p.o., BID)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02586155	Diabetes Mellitus, Type 2 ... more >> Coronary Artery Disease Cardiovascular Diseases Collapse <<	Phase 3	Recruiting	October 2018	Israel ... more >> Lady Davis Carmel Medical Center Recruiting Haifa, Israel, 34362 Contact: Basil Lewis, MD Collapse <<
NCT01067820	Coronary Artery Disease	Phase 2	Completed	-	-
NCT00768274	Dyslipidemia ... more >>Atherosclerosis Acute Coronary Syndrome Cardiovascular Disease Collapse <<	Phase 1 Phase 2	Completed	-	United States, Texas ... more >> Covance Clinical Research Unit, Inc. Dallas, Texas, United States, 75247 Collapse <<

更多
参考文献

[1] Picaud S, Wells C, 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] Bailey D, Jahagirdar R, 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 Jun 8;55(23):2580-9.
[3] Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H, Fedorov O, Müller S, Brennan PE, Knapp S, Filippakopoulos P. 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. doi: 10.1073/pnas.1310658110. Epub 2013 Nov 18. PMID: 24248379; PMCID: PMC3856850.
[4] Bailey D, Jahagirdar R, Gordon A, Hafiane A, Campbell S, Chatur S, Wagner GS, Hansen HC, Chiacchia FS, Johansson J, Krimbou L, Wong NC, Genest J. 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 Jun 8;55(23):2580-9. doi: 10.1016/j.jacc.2010.02.035. Erratum in: J Am Coll Cardiol. 2010 Aug 31;56(10):825. PMID: 20513599.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6998 mL
- 13.4990 mL
- 26.9979 mL
- 5 mM
- 0.5400 mL
- 2.6998 mL
- 5.3996 mL
- 10 mM
- 0.2700 mL
- 1.3499 mL
- 2.6998 mL

技术信息

CAS号

1044870-39-4

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H22N2O5

运输

蓝冰

分子量

370.40

别名

RVX-208;RVX000222;阿帕他隆

溶解度

DMSO	74.0 mg/mL (199.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02586155	Diabetes Mellitus, Type 2 ... more >> Coronary Artery Disease Cardiovascular Diseases Collapse <<	Phase 3	Recruiting	October 2018	Israel ... more >> Lady Davis Carmel Medical Center Recruiting Haifa, Israel, 34362 Contact: Basil Lewis, MD Collapse <<
NCT01067820	Coronary Artery Disease	Phase 2	Completed	-	-
NCT00768274	Dyslipidemia ... more >>Atherosclerosis Acute Coronary Syndrome Cardiovascular Disease Collapse <<	Phase 1 Phase 2	Completed	-	United States, Texas ... more >> Covance Clinical Research Unit, Inc. Dallas, Texas, United States, 75247 Collapse <<
NCT01423188	Coronary Artery Disease ... more >> Dyslipidemia Collapse <<	Phase 2	Completed	-	South Africa ... more >> East Burger Street, Bloemfontein, South Africa, 9301 Westdene, Bloemfontein, South Africa, 9301 Goodwood, Cape Town, South Africa, 7460 Kraaifontein, Cape Town, South Africa, 7570 Pinelands, Cape Town, South Africa, 7405 Chatsworth, Durban, South Africa, 4092` Congella, Durban, South Africa, 4001 Merebank, Durban, South Africa, 4052 Sydenham, Durban, South Africa, 4091 Tongaat, Durban, South Africa, 4400 Umhlanga, Durban, South Africa, 4321 Lenasia, Johannesburg, South Africa, 1827 Halfway House, Midrand, South Africa, 1685 Die Wilgers, Pretoria, South Africa, 0041 Eloffsdal, Pretoria, South Africa, 0084 Kuils River, Western Cape, South Africa, 7580 Parow, Western Cape, South Africa, 7500 Somerset West, Western Cape, South Africa, 7130 Stellenbosch, Western Cape, South Africa, 7600 Worcester, Western Cape, South Africa, 6850 Bloemfontein, South Africa, 9301 Cape Town, South Africa, 7505 Cape Town, South Africa, 7925 Johannesburg, South Africa, 1460 Western Cape, South Africa, 7646 Collapse <<
NCT03228940	Fabry Disease	Phase 1 Phase 2	Not yet recruiting	February 15, 2020	Canada, Nova Scotia ... more >> Queen Elizabeth II Health Sciences Centre, Victoria General Site Not yet recruiting Halifax, Nova Scotia, Canada, B3H2Y9 Contact: Michael West, MD (902) 473-4023 mwets@dal.ca Collapse <<
NCT03160430	Kidney Failure, Chronic	Phase 1 Phase 2	Not yet recruiting	March 15, 2020	-
NCT01728467	Diabetes	Phase 2	Completed	-	Australia, Victoria ... more >> Baker IDI Heart and Diabetes Institute 75 Commercial Road, Melbourne, Victoria, Australia, 3004 Collapse <<
NCT01863225	Dyslipidemia ... more >>Coronary Artery Disease Collapse <<	Phase 2	Terminated	-	Australia, South Australia ... more >> Royal Adelaide Hospital / CMAX Adelaide, South Australia, Australia, 5000 Collapse <<
NCT01058018	Atherosclerosis ... more >> Coronary Artery Disease Collapse <<	Phase 2	Completed	-	United States, California ... more >> Orange County Research Center Tustin, California, United States, 92780 Collapse <<

阿帕他隆 Catalog No. CSN13057

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