849662-80-2

Usage

Uses

Y 134 is a SERM displaying selectivity for ERα over ERβ.

Biological Activity

Selective estrogen receptor modulator (SERM) that displays selectivity for ER α over ER β (K i values are 0.09 and 11.31 nM respectively) and no cross-reactivity with mineralocorticoid, glucocorticoid, androgen and progesterone receptors. Acts as an agonist in the bone and antagonist in reproductive tissue. Suppresses estrogen-stimulated proliferation of ER-positive human breast cancer MCF-7 and T47D cells.

InChI:InChI=1/C28H28N2O3S/c1-18(2)29-13-15-30(16-14-29)21-7-3-19(4-8-21)27(33)26-24-12-11-23(32)17-25(24)34-28(26)20-5-9-22(31)10-6-20/h3-12,17-18,31-32H,13-16H2,1-2H3

Upstream product

• 849662-41-5 [4-(4-benzyl-piperazin-1-yl)-phenyl]-[6-methoxy-2-(4-methoxy-phenyl)-benzo[b]thiophen-3-yl]-methanone 
• 849662-42-6 (6-methoxy-2-(4-methoxyphenyl)benzo[b]thiophen-3-yl)(4-(piperazin-1-yl)phenyl)methanone 
• 206434-77-7 6-methoxy-2-(4-methoxyphenyl)-3-(4-fluorobenzoyl)benzo[b]thiophene 
• 63675-74-1 2-(4'-methoxyphenyl)-6-methoxybenzothiophene 
• 403-43-0 4-fluorobenzoyl chloride 
• 849662-58-4 [4-(4-isopropyl-piperazin-1-yl)-phenyl]-[6-methoxy-2-(4-methoxy-phenyl)-benzo[b]thiophen-3-yl]-methanone 

Relevant academic research and scientific papers

Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor α and their bioactivities in vivo

The synthesis of benzothiophenes containing a piperazine side chain and their binding affinities for estrogen receptors are described. These compounds bearing piperazine side chains were identified to be high-affinity ligands with high selectivity for ER