Estradiol valerate

Synonyms: E2V

Estradiol(E2V) is a synthetic ester used to treat menopausal symptoms and hormone deficiencies.

Estradiol valerate Chemical Structure

Estradiol valerate Chemical Structure

CAS: 979-32-8

Selleck's Estradiol valerate has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.83%
99.83

Choose Selective Estrogen/progestogen Receptor Inhibitors

Biological Activity

Description Estradiol(E2V) is a synthetic ester used to treat menopausal symptoms and hormone deficiencies.
Targets
ER [1]
In vitro
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. [1] 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. [2]

In Vivo
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. [3]

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

Chemical lnformation & Solubility

Molecular Weight 356.5 Formula

C23H32O3

CAS No. 979-32-8 SDF Download Estradiol valerate SDF
Smiles CCCCC(=O)OC1CCC2C1(CCC3C2CCC4=C3C=CC(=C4)O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 71 mg/mL ( (199.15 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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