2. Vitamin D Related/Nuclear Receptor Others
  3. Estrogen Receptor/ERR Drug Intermediate
  4. Estrogen receptor modulator 14

Estrogen receptor modulator 14 is a chromene-derived prodrug of selective Estrogen Receptor modulator with oral activity. Estrogen receptor modulator 14 undergoes hydrolysis in vivo to produce the active metabolite 2d-(R), which acts on ERα and ERβ. Estrogen receptor modulator 14 acts on central thermoregulatory sites and possesses the ability to regulate estrogen signaling in multiple systemic tissues. Estrogen receptor modulator 14 maintains antiestrogenic activity in the uterus, and alters plasma cholesterol and bone metabolism. Estrogen receptor modulator 14 can be used for the research of estrogen receptor-related diseases.

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Estrogen receptor modulator 14

Estrogen receptor modulator 14 Chemical Structure

CAS No. : 554429-88-8

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Estrogen receptor modulator 14 Related Antibodies

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Description

Estrogen receptor modulator 14 is a chromene-derived prodrug of selective Estrogen Receptor modulator with oral activity. Estrogen receptor modulator 14 undergoes hydrolysis in vivo to produce the active metabolite 2d-(R), which acts on ERα and ERβ. Estrogen receptor modulator 14 acts on central thermoregulatory sites and possesses the ability to regulate estrogen signaling in multiple systemic tissues. Estrogen receptor modulator 14 maintains antiestrogenic activity in the uterus, and alters plasma cholesterol and bone metabolism. Estrogen receptor modulator 14 can be used for the research of estrogen receptor-related diseases[1].

Cellular Effect
Cell Line Type Value Description References
Ishikawa IC50
175 nM
Compound: 1-(R)
Inhibition of estrogen receptor in Ishikawa cells
Inhibition of estrogen receptor in Ishikawa cells
[PMID: 16722623]
MCF7 IC50
510 nM
Compound: 1-(R)
Inhibition of estrogen receptor in MCF7 cells
Inhibition of estrogen receptor in MCF7 cells
[PMID: 16722623]
In Vitro

Estrogen receptor modulator 14 (1-(R)) does not bind to purified estrogen receptor α and estrogen receptor β, with an IC50 >10000 nM[1].
Estrogen receptor modulator 14 exerts anti-estrogenic activity in human endometrial Ishikawa cells, with an IC50 value of 175 nM[1].
Estrogen receptor modulator 14 exerts anti-estrogenic activity in human breast cancer MCF-7 cells, with an IC50 of 510 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Estrogen receptor modulator 14 Related Antibodies
In Vivo

Estrogen receptor modulator 14 (1-(R)) (0.14-1.4 mg/kg; p.o.; once daily; for 3 consecutive days) dose-dependently inhibits estrone-induced uterine weight gain in immature rats, while exhibiting no intrinsic uterine stimulatory activity[1].
Estrogen receptor modulator 14 (0.042-1.4 mg/kg; p.o.; daily; 2-6 weeks) acts as an estrogen agonist in ovariectomized rats, preventing bone loss, reducing total cholesterol, and increasing vaginal secretions, while exhibiting anti-estrogenic activity in the uterus[1].
Estrogen receptor modulator 14 (0.14-4.2 mg/kg; p.o.; daily) effectively inhibits the tail skin temperature elevation resembling hot flashes in drug-dependent rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Immature rats[1]
Dosage: 0.14 mg/kg; 0.42 mg/kg; 1.4 mg/kg
Administration: p.o.; daily; 3 days
Result: Inhibited estrone-stimulated uterine weight increase by 27% at 0.14 mg/kg.
Inhibited estrone-stimulated uterine weight increase by 55% at 0.42 mg/kg.
Inhibited estrone-stimulated uterine weight increase by 75% at 1.4 mg/kg.
Showed no significant agonistic activity to stimulate uterine growth when administered alone at 1.4 mg/kg.
Animal Model: Adult ovariectomized rats[1]
Dosage: 0.042 mg/kg; 0.14 mg/kg; 1.4 mg/kg (vaginal fluid endpoint)
Administration: p.o.; daily; 2 weeks (vaginal fluid endpoint); daily
Result: Prevented ovariectomy-induced bone loss in a dose-dependent manner (to a level similar to raloxifene) over 6 weeks of treatment.
Reduced circulating serum total cholesterol levels at all tested doses, with maximum reduction to approximately 33-35% of vehicle-treated control levels over 6 weeks of treatment.
Increased vaginal fluid weight in ovariectomized rats at 0.14 mg/kg/day and 1.4 mg/kg/day doses after 2 weeks of treatment.
Molecular Weight

639.79

Formula

C39H45NO7
CAS No.
SMILES

O(C(C(C)(C)C)=O)C=1C=C2C(C3=C(C=4C(O[C@@H]3C5=CC=C(OCCN6CCCCC6)C=C5)=CC(OC(C(C)(C)C)=O)=CC4)CO2)=CC1
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Purity & Documentation
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Estrogen receptor modulator 14 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Estrogen receptor modulator 14554429-88-8Estrogen receptor modulator14Estrogen receptor modulator-14Estrogen Receptor/ERRDrug IntermediateDrug Iintermediateestrogen receptor βimmature ratsthermoregulatory centerIshikawa human endometrial cellsMCF-7 human breast cancer cellsvaginaestrogen receptor αmorphine-dependent ratsuterusovariectomized ratsInhibitorinhibitorinhibit

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