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
Y 134 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
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
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
Keywords: Y 134, supplier, Selective, estrogen, receptor, modulators, SERM, selective, Erα, Eralpha, ERR, Estrogen, Receptors, Y134, Estrogen, and, Related, Receptors, Estrogen, and, Related, Receptors, Tocris Bioscience
