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Chemical Structure : RVX-208
CAS No.: 1044870-39-4
Catalog No.: 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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| 100 mg | $528 | In stock | |
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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.
| M.Wt | 370.405 | |
| Formula | C20H22N2O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-4(3H)-quinazolinone |
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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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