Apabetalone
Cat. No.:YN250672
CAS No. :1044870-39-4
产品名称: | Apabetalone |
CAS No.: | 1044870-39-4 |
Chemical Name: | 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-4(3H)-quinazolinone |
Synonyms: | 阿帕他隆; RVX-208; RVX000222 |
分子量: | 370.40 |
分子式: | C₂₀H₂₂N₂O₅ |
SMILES: | COC1=CC(OC)=C(C(NC(C2=CC(C)=C(OCCO)C(C)=C2)=N3)=O)C3=C1 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Apabetalone (RVX-208) 是一种BET转录抑制剂,作用于BD1和BD2,IC50分别为 87±10 μM 和 0.51±0.041 μM。 |
IC50和靶点: | |
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Filippakopoulos, P., Qi, J., Picaud, S., et al.Selective inhibition of BET bromodomainsNature468(7327),1067-1073(2010)
McLure, K.G., Gesner, E.M., Tsujikawa, L., et al.RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonistPLoS One8(12),1-12(2013)
Picaud, S., Wells, A., Felletar, I., et al.RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomainProc. Natl. Acad. Sci. USA110(49),19754-19759(2013)
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 vivoJ. Am. Coll. Cardiol.55(23),2580-2589(2010)
Jahagirdar, R., Zhang, H., Azhar, S., et al.A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient miceAtherosclerosis236(1),91-100(2014)