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Estradiol

Sex Hormones & TRT
E217β-EstradiolEstradiol ValerateEstrofemClimaraDivigel

Overview

Estradiol, also known as E2, 17β-Estradiol, or Estradiol Valerate, is a predominant form of estrogen, an endogenous steroid hormone. It is primarily produced in the ovaries, but also in smaller amounts by the adrenal glands and in adipose tissue. Chemically, it belongs to the class of compounds known as estrogens, which are a group of steroid hormones. Estradiol is also synthesized for medical use, often in the form of various esters such as estradiol valerate. Researchers have extensively studied its role in the development and regulation of the female reproductive system and secondary sexual characteristics. Estradiol plays a critical role in the menstrual cycle and is involved in the regulation of the estrous and menstrual reproductive cycles. It has been the focus of research in areas such as bone density, cardiovascular health, and neuroprotection. The mechanism of action of estradiol involves binding to estrogen receptors, ERα and ERβ, which are distributed throughout various tissues in the body. Upon binding, these receptors act as transcription factors that regulate the expression of genes involved in cell growth, differentiation, and reproductive function. Estradiol's pharmacokinetic properties vary depending on the route of administration. Endogenously, it has a circulating half-life of approximately 70 minutes. When administered orally, its bioavailability is reduced due to first-pass metabolism. Transdermal and injectable forms, such as estradiol valerate, offer different pharmacokinetic profiles, often with longer half-lives. Clinically, estradiol is used in hormone replacement therapy, contraceptive formulations, and in the treatment of menopausal symptoms. It is regulated as a prescription medication in many countries, reflecting its significant physiological effects and potential side effects. Researchers have observed its efficacy in these clinical applications, although its use must be carefully managed under medical supervision.

Mechanism of Action

Estradiol acts primarily on estrogen receptors ERα and ERβ, which are nuclear receptors that, upon activation, regulate gene expression. This activation leads to a cascade of biological events that influence reproductive tissue development, bone density, and cardiovascular function.

Molecular Data

FormulaC18H24O2
Molecular Weight272.4 g/mol
CAS Number50-28-2
PubChem CID5757

Half-Life & Pharmacokinetics

EndogenousCirculating half-life ~70 minutes
Intramuscular~7-10 days (valerate ester)
TransdermalSteady-state after 24-48h
OralPoor bioavailability due to first-pass metabolism

Different esters of estradiol, such as valerate and cypionate, have varying half-lives and pharmacokinetic profiles.

Storage

Temperature

Store at room temperature (15-30°C)

Light

Protect from light

Form

Oil solution stable for 2+ years

Notes

Avoid freezing; ensure container is tightly closed.

Solubility

Estradiol is poorly soluble in water but soluble in ethanol and oils, which is relevant for its formulation in various delivery methods.

Legal Status

🇩🇪DE

Prescription only (verschreibungspflichtig); not a controlled substance under BtMG.

🇺🇸US

FDA approved for various indications; prescription required; not a controlled substance.

🇦🇺AU

TGA Schedule 4 (prescription only medicine).

🇬🇧UK

Prescription only medicine (POM) under MHRA regulations.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

10 Research Publications

17β-estradiol ameliorates LPS-induced acute lung injury via mediating mitochondrial biogenesis and function in rats.

Animal

International immunopharmacology · 2025

Researchers found that the hormone 17β-estradiol (E2) can help protect against lung damage caused by sepsis in rats. They observed that E2 improves mitochondrial function and reduces cell death, suggesting it could be a potential treatment for severe lung conditions like acute respiratory distress syndrome.

  • E2 deficiency worsens lung injury and mitochondrial damage.
  • Exogenous E2 reverses lung injury effects.
  • E2 promotes mitochondrial health through specific signaling pathways.
PubMed

17β-estradiol in colorectal cancer: friend or foe?

Review

Cell communication and signaling : CCS · 2024

Researchers observed that 17β-Estradiol (E2) may play a complex role in colorectal cancer (CRC), potentially reducing risk in women by inhibiting cancer cell growth and promoting a less favorable environment for tumor development. However, under certain stressful conditions, E2 could also contribute to cancer progression, highlighting its dual nature in CRC.

  • E2 may reduce CRC risk in women by inhibiting cancer cell proliferation and migration.
  • E2 can create an unfavorable tumor environment by reducing inflammation and altering gut microbiome.
  • Under high stress conditions, E2 might promote CRC development through different signaling pathways.
PubMed

17β-estradiol biosensors based on different bioreceptors and their applications.

Review

Frontiers in bioengineering and biotechnology · 2024

Researchers observed that 17β-estradiol (E2) is an important hormone affecting both humans and animals. They found that biosensors, which are small and efficient devices, can effectively detect E2 in various settings, including environmental monitoring and food safety. The review highlights different types of biosensors and their applications in ensuring safety and detecting diseases.

  • Biosensors can quickly and accurately detect E2 with minimal samples.
  • Different types of biosensors include non-biometric, enzyme, antibody, and aptamer biosensors.
  • Applications of E2 detection span environmental monitoring, food safety, and medical safety.
PubMed

Biotransformation of 17β-Estradiol through a Denitrifying Sludge.

Unknown

International journal of environmental research and public health · 2022

Researchers observed that 17β-estradiol, a natural estrogen harmful to aquatic life, can be effectively broken down using denitrifying sludge. This biological process shows promise for treating water contaminated with this substance, ensuring its complete removal from the environment.

  • Denitrifying sludge can biodegrade 17β-estradiol.
  • The process may help eliminate harmful estrogen from polluted water.
  • This method has previously been successful in degrading other drugs.
PubMed

Estradiol induces synaptic rearrangements.

Unknown

Vitamins and hormones · 2020

Researchers observed that the hormone 17β-Estradiol (E2) plays a significant role in the formation and rearrangement of synapses in the brain, particularly in areas related to learning and memory. They highlighted the molecular mechanisms by which E2 influences these changes and suggested that it may work alongside other substances, like adenosine, to enhance brain plasticity.

  • E2 affects synaptic plasticity in brain regions important for learning and memory.
  • The hormone influences the formation and rearrangement of dendritic spines.
  • E2 may have synergistic effects with other synaptic modulators like adenosine.
PubMed

Xenoestrogen regulation of ERα/ERβ balance in hormone-associated cancers.

Review

Molecular and cellular endocrinology · 2017

Researchers observed that the hormone 17β-estradiol (E2) plays a crucial role in regulating various body functions through two estrogen receptors, ERα and ERβ. They found that the balance between these receptors is important in cancer development and that certain chemicals, known as xenoestrogens, can disrupt this balance, potentially influencing cancer progression related to E2.

  • The ratio of estrogen receptors ERα and ERβ is vital for understanding cancer progression.
  • Xenoestrogens can interfere with the normal signaling of estrogen receptors.
  • Disruption of E2 signaling by xenoestrogens may contribute to the development of hormone-associated cancers.
PubMed

Immunomodulation by the estrogen metabolite 2-methoxyestradiol.

Human

Clinical immunology (Orlando, Fla.) · 2014

Researchers observed that 2-methoxyestradiol (2me2), a compound related to estrogen, affects the immune system in a dose-dependent manner. They found that lower doses of 2me2 increased certain immune cells, while higher doses had effects similar to estrogen. Overall, estrogen had a stronger impact on immune regulation than 2me2.

  • Lower doses of 2me2 increased immune cells in mice.
  • Higher doses of 2me2 had effects similar to estrogen.
  • Estrogen was more effective in regulating the immune system than 2me2.
PubMed

Estrogen and cerebrovascular regulation in menopause.

Review

Molecular and cellular endocrinology · 2014

Researchers observed that estrogen plays important roles beyond reproduction, including protecting the brain and blood vessels. They found that lower estrogen levels during menopause are linked to increased risks of brain and blood vessel diseases, and the effects of hormone therapy are still debated. The review highlights the potential benefits of estrogen in brain health and discusses the timing of hormone therapy's effectiveness.

  • Lower estrogen levels during menopause are associated with higher risks of cerebrovascular and neurological diseases.
  • The effects of menopausal hormone therapy on brain health and stroke risk are controversial.
  • Emerging evidence suggests that the timing of hormone therapy may influence its protective effects on the brain.
PubMed

Xenoestrogens challenge 17β-estradiol protective effects in colon cancer.

Review

World journal of gastrointestinal oncology · 2014

Researchers observed that environmental chemicals known as xenoestrogens may interfere with the protective effects of the hormone 17β-estradiol (E2) against colorectal cancer. They highlighted that while E2 plays a significant role in cancer prevention, the impact of xenoestrogens on E2's function is not well understood, particularly in relation to gender differences and age.

  • Xenoestrogens may disrupt the protective actions of E2 in colorectal cancer.
  • E2 is crucial for understanding sex differences in cancer risk.
  • There is limited knowledge about E2's role in preventing colorectal cancer.
PubMed

Role of 17β-estradiol and testosterone in apoptosis.

Review

Steroids · 2011

Researchers observed that the hormones 17β-estradiol (E2) and testosterone (T) play important roles in regulating cell death, known as apoptosis, in various tissues. They found that these hormones can protect mitochondria, the energy centers of cells, from damage, which helps prevent cell death.

  • E2 and T affect growth and cell functions in many organs beyond the reproductive system.
  • Both hormones can activate signaling pathways quickly, influencing cell survival.
  • E2 and T primarily protect mitochondria, contributing to their anti-apoptotic effects.
PubMed

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This page is for informational and research purposes only. All information is based on published scientific literature. Nothing on this page constitutes medical advice or replaces consultation with a qualified healthcare professional.