research use only
Cat.No.S3149
| Related Targets | Adrenergic Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR |
|---|---|
| Other Estrogen/progestogen Receptor Inhibitors | Elacestrant (RAD1901) Dihydrochloride MPP dihydrochloride Cholesterol Endoxifen HCl G15 Chrysin Licochalcone A AZD9496 PHTPP Liquiritigenin |
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In vitro |
DMSO
: 71 mg/mL
(199.15 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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| Molecular Weight | 356.5 | Formula | C23H32O3 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 979-32-8 | Download SDF | Storage of Stock Solutions |
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| Synonyms | E2V | Smiles | CCCCC(=O)OC1CCC2C1(CCC3C2CCC4=C3C=CC(=C4)O)C | ||
| Targets/IC50/Ki |
ER
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|---|---|
| In vitro |
Estradiol (10 nM) rapidly activates sphingosine kinase isoenzyme SphK1 as determined by enhanced phosphorylation on Ser225 in MCF-7 cells. Estradiol (20 nM) stimulates rapid release of sphingosine 1-phosphate (S1P) and dihydro-S1P from MCF-7 cells. SphK1 and estrogen receptor α are mainly responsible for formation of S1P and dihydro-S1P. Down-regulation of ABCC1 or ABCG2 with siRNAs or pharmacological inhibitors decreases Estradiol (10 nM)-mediated release of S1P or dihydro-S1P from MCF-7 cells. Estradiol (10 nM) inhibits miR-21 expression in MCF-7 human breast cancer cells mediated by estrogen receptor α. Estradiol (10 nM) activates several miR-21 target gene reporters activity in MCF-7 cells through inhibiting miR-21 expression. Estradiol (10 nM) increases endogenous miR-21 target genes expression in protein but not RNA levels in MCF-7 cells. |
| In vivo |
Estradiol (80 μg/kg/day, s.c.) significantly decreases the absolute numbers of total peritoneal cell and macrophages, characterized by a double F4/80- and CD11b-positive staining, in ovariectomized C57BL/6J mice. Estradiol (80 μg/kg/day, s.c.) enhances the LPS-induced expression of proinflammatory cytokines by TGC-elicited macrophages through inhibition of PI3K activity in ovariectomized C57BL/6J mice. Proinflammatory effect of Estradiol is abolished by downregulate estrogen receptor α activity in thioglycolate-elicited macrophages. |
References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04901377 | Completed | Oral Contraception |
Bayer |
June 24 2021 | -- |
| NCT00463450 | Completed | Hormone Replacement Therapy |
Bayer|Navitas Life Sciences GmbH|LKF Laboratory |
May 2002 | Phase 3 |
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