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Art. -Nr.: HY-107076

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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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CAS. Nr.: 554429-88-8
Formel: C₃₉H₄₅NO₇
Molecular Weight:639.79

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Please store the product under the recommended conditions in the Certificate of Analysis.

Estrogen receptor modulator 14 Chemical Structure

CAS. Nr.: 554429-88-8

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
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Bioz

Biologische Aktivität

Beschreibung

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

CAS. Nr. 554429-88-8
Molecular Weight 639.79
Formel C₃₉H₄₅NO₇
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Jain N, et al. Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness. Journal of medicinal chemistry. 2006 Jun 01;49(11):3056-9. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Estrogen receptor modulator 14

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Estrogen receptor modulator 14

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

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Calculators

Help & FAQs

Estrogen receptor modulator 14 Related Classifications

HY-107076 Related Classifications