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Estradiol is a white or creamy-white or non-crystalline powder, soluble in dioxane and acetone, slightly soluble in ethanol and insoluble in water. Estradiol is an intermediate between estradiol valerate and estradiol benzoate, an estrogenic drug. It is used to treat functional uterine bleeding, primary amenorrhoea, menopausal syndrome and prostate cancer. Estradiol promotes and regulates the normal growth of female sex organs and secondary sex characteristics, promotes the maturation and growth of breast ducts, and helps in positioning. Estradiol is also used in biochemical studies.
Uses and functions of Estradiol.
Estradiol is used as an oestrogenic drug for functional uterine bleeding, primary amenorrhoea, menopausal syndrome and prostate cancer.
It can promote and regulate the normal development of female sex organs and secondary sex characteristics. It can promote the development of breast ducts and hyperplasia, but at higher doses, it can inhibit the release of prolactin from the anterior pituitary gland and reduce milk secretion.
It can also be used to return milk. But there may be nausea, vomiting and endometrial hyperplasia and bleeding. Use with caution in hepatic and renal insufficiency. Contraindicated for use on breasts, vulva and vaginal mucosa.
Pharmacological Effect of Estradiol Powder.
Estradiol is an estrogen with high receptor level activity secreted by the ovaries of women of childbearing age. After menopause, the ovaries fail and the production of oestradiol almost stops, thus causing vasomotor disorders, instability of thermoregulation, and clinical symptoms such as hot flushes, sweating, sleep disorders, atrophy of the genitourinary system and osteoporosis.
The absorption of oestradiol into the blood increases the concentration of oestradiol in the blood to the level of early follicular stage, which acts on the target organs, thus causing the above symptoms to be significantly reduced or disappeared.
Product Method of Bulk Estradiol Powder.
The product was produced from androst-4-ene-19-demethyl-3,17-dione by bromination to introduce bromine at the 2- and 6-positions, followed by debromination (elimination) in the presence of 4-ethyl-2-methylpyridine to produce 2,4,6-androstatriene-19-demethyl-3,17-dione, which was then subjected to high-temperature cleavage to produce estrone, which was then reduced with lithium-aluminium-hydrogen to produce the product.
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