Raw material β-Estradiol powder Estradiol enanthaye CAS 50-28-2 and Estradiol

  Product Detail  

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MF C25H28O3
MW 376.5
EINECS NO. 200-043-7
Melting Point 191-198 °C(lit.)
Boiling Point 465.03°C (rough estimate)
Density 1.0493 (rough estimate)
Storage 2-8°C

Description Estradiolbenzoate is a synthetic ester, especially 3-benzoyl ester, natural estrogen, estradiol. Estrogens guides the development of female genes during embryonic development and puberty. Estradiol is the main female hormone secreted by the ovaries before menopause. Estradiolbenzoat Chemicalbooke is an estradiol analogue that contains a benzyl ester at the C-3 position and is often used in combination with progesterone to induce estrus in livestock. The compound binds to human and mouse estrogen receptor alpha (ERα), and chicken ER, with IC50 values ranging from 22-28 nM.

This reflects a 6-10 fold reduction in affinity compared to estradiol.
Application The effects of daily injections of 5 microgram estradiol benzoate (EB) on the patterns of food and ethano consumption were studied in ovarectomized rats given free access to food, a 10% ethano solution, and water. EB led to an immediate, but transient, suppression of both food and ethano intake. The time course and magnitude of these effects were virtually identical. While the decrease in total food intake was achieved by a permanent decrease in the duration of eating bouts, the decline in total ethano consumption apparently resulted from decreased rates of licking within bouts.

Gradual increases in the frequency of eating and ethano-drinking bouts allowed total food and ethano intake to return to baseline within three weeks of the first injection. Total water intake rose three-fold during EB administration and this was due to increases in both the duration and frequency of drinking bouts. The similarity in effects induced by EB on the patterns of food and ethano intake were discussed in terms of ethano's caloric property.

• Estradiol, also known as 17β-estradiol or 17β-oestradiol, is a naturally occurring steroid hormone and the most potent form of estrogen in mammals. It is primarily produced in the ovaries, but also synthesized in smaller amounts by other tissues such as the adrenal glands and fat cells. Estradiol plays a crucial role in various physiological processes, particularly in the development and maintenance of female reproductive tissues, secondary sexual characteristics, and overall reproductive health
  

  Mechanism of Action

  Estradiol exerts its effects primarily through binding to estrogen receptors (ERs), specifically estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ). These receptors are nuclear hormone receptors that, upon binding with estradiol, form dimers and translocate to the nucleus where they regulate gene transcription. This process involves:
  1. Binding: Estradiol binds to ERα and ERβ, initiating a cascade of cellular responses.
  2. Gene Regulation: The ER-ligand complex interacts with specific DNA sequences to modulate the expression of target genes involved in various physiological functions including reproduction, bone density, and cardiovascular health.
  3. Rapid Effects: Estradiol also acts on G Protein-coupled Estrogen Receptor (GPER), mediating rapid non-genomic effects such as vasodilation

  Applications

  1. Menopausal Symptom Relief
  Treats moderate to severe vasomotor symptoms (hot flashes, night sweats) due to menopause
  Treats vulvar and vaginal atrophy (dryness, itching, burning) due to menopause
  2. Osteoporosis Prevention
  Prevents postmenopausal osteoporosis by inhibiting bone resorption and increasing bone density
  3. Hormone Replacement Therapy (HRT)
  Treats hypoestrogenism due to hypogonadism, castration, or primary ovarian failure
  4. Cancer Treatment
  Used for palliation therapy of certain types of breast cancer in men and women with metastatic disease
  Used for palliation therapy of androgen-dependent prostate cancer
  5. Contraception
  Used in combination with other hormones as a component of oral contraceptive pills to prevent pregnancy

  Routes of Administration

  Estradiol can be administered through various routes:
  1. Oral Tablets: Common but subject to first-pass metabolism, reducing bioavailability (2-10%).
  2. Transdermal Patches: Bypass first-pass metabolism and provide steady hormone levels.
  3. Vaginal Preparations: Such as creams or rings that allow for direct absorption into the bloodstream without liver metabolism.
  4. Injectable Forms: Including intramuscular injections that provide longer-lasting effects due to depot formulations

  Safety and Side Effects

  While estradiol therapy can be beneficial, it is not without risks. Potential side effects include:
  1. Cardiovascular Risks: Increased risk of thromboembolic events and stroke, particularly in women with pre-existing conditions.
  2. Hormonal Side Effects: Nausea, headaches, and breast tenderness are common.

  3. Cancer Risks: Long-term use may increase the risk of endometrial and breast cancer.