Y 134A SERM displaying selectivity for ERα over ERβ

Y 134 (CAS 849662-80-2)

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Synonym: [6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl]-[4-[4-(1-methylethyl)-1-piperazinyl]phenyl]methanone
Application: A SERM displaying selectivity for ERα over ERβ
CAS Number: 849662-80-2
Purity: ≥98%
Molecular Weight: 472.60
Molecular Formula: C28H28N2O3S
* Refer to Certificate of Analysis for lot specific data (including water content).
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Y 134 is a selective estrogen receptor modulator (SERM), selective for ERα. Non cross-reactive with mineralocorticoid, glucocorticoid, androgen, and progesterone receptors. Y 134 exhibits agonist behaviors in bone and antagonist behavior in reproductive tissue. Y 134 decreases activity of estrogen-stimulated proliferation of ER+ human breast cancer MCF-7 and T47D cells.


References

Yang et al (2005) Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor a and their bioactivities in vivo. Bioorg.Med.Chem.Lett. 15 1505. Ning et al (2007) Biological activities of a novel selective oestrogen receptor modulator derived from raloxifene (Y134). Br.J.Pharmacol. 150 19.

Physical State :
Solid
Solubility :
Soluble in ethanol (100 mM), and DMSO (100 mM).
Storage :
Desiccate at room temperature
Melting Point :
287.02° C (Predicted)
Boiling Point :
~722.3° C at 760 mmHg (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.67 (Predicted)
IC50 :
ERα: IC50 = 0.28 nM (human); ERβ: IC50 = 33.92 nM (human)
Ki Data :
ERα: Ki= 0.09 nM; ERβ: Ki= 11.31 nM
pK Values :
pKa: 8.93 (Predicted), pKb: 8.19 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
11784736
MDL Number :
MFCD09970973
SMILES :
CC(C)N1CCN(CC1)C2=CC=C(C=C2)C(=O)C3=C(SC4=C3C=CC(=C4)O)C5=CC=C(C=C5)O

Download SDS (MSDS)

Certificate of Analysis

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