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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 554429-88-8
- Formule: C39H45NO7
- Masse moléculaire:639.79
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
|
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] |
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 (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 No. 554429-88-8
-
Masse moléculaire 639.79
-
Formule 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
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Estrogen receptor modulator 14 Related Classifications
HY-107076 Related Classifications
Powered by Bioz
- Estrogen receptor modulator 14
- 554429-88-8
- Estrogen receptor modulator14
- Estrogen receptor modulator-14
- Estrogen Receptor/ERR
- Drug Intermediate
- estrogen receptor β
- immature rats
- thermoregulatory center
- Ishikawa human endometrial cells
- MCF-7 human breast cancer cells
- vagina
- estrogen receptor α
- morphine-dependent rats
- uterus
- ovariectomized rats
- Inhibitor
- inhibitor
- inhibit