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Estradiol valerate Estrogen/progestogen Receptor agonist

Cat.No.S3149

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

Batch: Purity: 99.83%
99.83

Solubility

In vitro
Batch:

DMSO : 71 mg/mL (199.15 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous 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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 356.5 Formula

C23H32O3

Storage (From the date of receipt)
CAS No. 979-32-8 Download SDF Storage of Stock Solutions

Synonyms E2V SMILES CCCCC(=O)OC1CCC2C1(CCC3C2CCC4=C3C=CC(=C4)O)C

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
ER
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
  • [4] https://pubmed.ncbi.nlm.nih.gov/15820610/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-02-02)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07041814 NOT_YET_RECRUITING
Turner Syndrome
Universiti Kebangsaan Malaysia Medical Centre
2026-02-15 PHASE2
NCT07419594 RECRUITING
PTSD; Intrusive Memories; Intrusion Symptom; Trauma; Intrusion
Charite University, Berlin, Germany
2024-08-19
NCT07379502 NOT_YET_RECRUITING
PCOS (Polycystic Ovary Syndrome)
CMH Kharian Medical College
2026-03-05
NCT07727863 COMPLETED
PCOS GnRH Antagonist and GnRH Agonist IVF/ICSI Cycles; IVF Outcomes
Cairo University
2024-09-13
NCT03976544 TERMINATED
Miscarriage; Frozen Embryo Transfer; Natural Cycle; Hormone Replacement Therapy Cycle; Preimplantation Genetic Screening; Euploid Embryos
CRG UZ Brussel
2019-05-25 PHASE4
NCT02330757 UNKNOWN
Infertility
Mansoura University
2016-10-10 PHASE4

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