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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-RVX-208
RVX-208

Chemical Structure : RVX-208

CAS No.: 1044870-39-4

RVX-208 (Apabetalone, RVX-000222)

货号: PC-49079Not For Human Use, Lab Use Only.

Apabetalone (RVX-208) is a potent, selective inhibitor of second BET bromodomains (BD2) with IC50 of 0.51 uM, 170-fold selectivity over BD1 (IC50=87 uM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Apabetalone (RVX-208) is a potent, selective inhibitor of second BET bromodomains (BD2) with IC50 of 0.51 uM, 170-fold selectivity over BD1 (IC50=87 uM).
Apabetalone (RVX-208) exhibits a KD of 4.06 ± 0.16 μM for BD1 and more than 20-fold stronger binding to BD2 (0.194 ± 0.013 μM) in the case of BRD3.
Apabetalone (RVX-208) displaces BET proteins from chromatin.
Apabetalone (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 through an epigenetic mechanism.
Apabetalone (RVX-208) downregulates expression of cell surface receptors involved in SARS-CoV-2 entry, including angiotensin-converting enzyme 2 (ACE2) and dipeptidyl-peptidase 4 (DPP4 or CD26) in SARS-CoV-2 permissive cells, inhibits SARS-CoV-2 infection in vitro.

物理化学性质&存储条件

分子量 370.405
分子式 C20H22N2O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Picaud S, et al. Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9.

2. McLure KG, et al. PLoS One. 2013 Dec 31;8(12):e83190.

3. Gilham D, et al. Atherosclerosis. 2016 Apr;247:48-57.

4. Gilham D, et al. Biomedicines. 2021 Apr 18;9(4):437.

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