| Identification | Back Directory | [Name]
Y 134 | [CAS]
849662-80-2 | [Synonyms]
Y 134
[6-HYDROXY-2-(4-HYDROXYPHENYL)BENZO[B]THIEN-3-YL]-[4-[4-(1-METHYLETHYL)-1-PIPERAZINYL]PHENYL]METHANONE
Methanone, [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[4-(1-methylethyl)-1-piperazinyl]phenyl]- | [Molecular Formula]
C28H28N2O3S | [MDL Number]
MFCD09970973 | [MOL File]
849662-80-2.mol | [Molecular Weight]
472.6 |
| Chemical Properties | Back Directory | [storage temp. ]
Desiccate at RT | [solubility ]
Soluble to 100 mM in DMSO and to 100 mM in ethanol | [form ]
Powder | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Y 134 is a SERM displaying selectivity for ERα over ERβ. | [Definition]
ChEBI: [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(4-propan-2-yl-1-piperazinyl)phenyl]methanone is an aromatic ketone. | [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. | [in vivo]
Y134 (1-3 mg/kg/day; p.o. for 3 days) abolishes the E2-induced mammary gland terminal end bud (TEB) outgrowth in ovariectomized rats. Y134 inhibits uterine cell proliferation induced by E2 in a dose-dependent manner[1]. | Animal Model: | Four-week old female Sprague-Dawley rats were received ovariectomy[1] | | Dosage: | 1, 3 mg/kg | | Administration: | P.o. daily for 3 days | | Result: | Abolished the effect exerted by E2 in a dose-dependent manner.
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| [IC 50]
ERα: 0.09 nM (Ki); ERβ: 11.31 nM (Ki) | [storage]
Desiccate at RT |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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