Y 134

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Cat.No. 2676 - Y 134 | C28H28N2O3S | CAS No. 849662-80-2
Description: Selective estrogen receptor modulator (SERM), selective for ERα
Chemical Name: [6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl]-[4-[4-(1-methylethyl)-1-piperazinyl]phenyl]methanone
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature
Pathways

Biological Activity

Selective estrogen receptor modulator (SERM) that displays selectivity for ERα over ERβ (Ki 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.

Compound Libraries

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Technical Data

M. Wt 472.6
Formula C28H28N2O3S
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 849662-80-2
PubChem ID 11784736
InChI Key LQEOPHGPHCWOAC-UHFFFAOYSA-N
Smiles CC(C)N1CCN(CC1)C1=CC=C(C=C1)C(=O)C1=C(SC2=CC(O)=CC=C12)C1=CC=C(O)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 47.26 100
ethanol 47.26 100

Preparing Stock Solutions

The following data is based on the product molecular weight 472.6. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.12 mL 10.58 mL 21.16 mL
5 mM 0.42 mL 2.12 mL 4.23 mL
10 mM 0.21 mL 1.06 mL 2.12 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Yang et al (2005) Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor α and their bioactivities in vivo. Bioorg.Med.Chem.Lett. 15 1505 PMID: 15713417

Ning et al (2007) Biological activities of a novel selective oestrogen receptor modulator derived from raloxifene (Y134). Br.J.Pharmacol. 150 19 PMID: 17115070


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Pathways for Y 134

Estrogen

Estrogen Signaling Pathway

Estrogen is a steroid hormone that is responsible for the regulation of growth, differentiation and function of the reproductive system. Estrogen signaling is often dysregulated in breast cancer and osteoporosis.