DCW234
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DCW234, also known as butyl 4-(butyryloxy)benzoate, is a
synthetic Synthetic things are composed of multiple parts, often with the implication that they are artificial. In particular, 'synthetic' may refer to: Science * Synthetic chemical or compound, produced by the process of chemical synthesis * Synthetic ...
nonsteroidal A nonsteroidal compound is a drug that is not a steroid nor a steroid derivative. Nonsteroidal anti-inflammatory drugs (NSAIDs) are distinguished from corticosteroids as a class of anti-inflammatory agents. List of nonsteroidal steroid receptor mo ...
estrogen Estrogen or oestrogen is a category of sex hormone responsible for the development and regulation of the female reproductive system and secondary sex characteristics. There are three major endogenous estrogens that have estrogenic hormonal ac ...
and a selective
agonist An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ag ...
of the ERβ. It shows modest selectivity in terms of affinity and
transactivation In the context of gene regulation: transactivation is the increased rate of gene expression triggered either by biological processes or by artificial means, through the expression of an intermediate transactivator protein. In the context of recep ...
for the ERβ over the ERα. Its affinity for the ERβ was 3.43 μM and for the ERα was 22.5 μM, while it activated the ERβ and ERα with EC50 values of 1.71–2.5 μM and 19.8–22.5 μM, respectively. As such, its binding selectivity for the ERβ over the ERα was 7-fold and its
functional selectivity Functional selectivity (or “agonist trafficking”, “biased agonism”, “biased signaling”, "ligand bias" and “differential engagement”) is the ligand-dependent selectivity for certain signal transduction pathways relative to a referen ...
for the ERβ over the ERα was between 10- and 13-fold.


See also

*
Diarylpropionitrile Diarylpropionitrile (DPN), also known as 2,3-bis(p-hydroxyphenyl)propionitrile (2,3-BHPPN), is a synthetic, nonsteroidal, and highly selective agonist of ERβ ( IC50 = 15 nM) that is used widely in scientific research to study the function o ...


References

{{Estrogen receptor modulators Benzoate esters Selective ERβ agonists Synthetic estrogens