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|Product Name:||Estriol||Appearance:||White Powder|
pharmaceutical active ingredients,
pharmaceutical fine chemicals
Pharmaceutical Raw Steroid Powder Estriol CAS 50-27-1 For Treatment Of Female Hormone
Estriol belongs to natural hormone and is the metabolite of estradiol in vivo , anti estrogen steroids . It is mainly presented in the urine . Estrogen has a relative small activity with the oral activity being 6 times as high as estrone but being weaker than estradiol with non-carcinogenic effects . After its administration , the in vivo estradiol levels did not change . Estriol has selective action on the vaginal and cervical canal but has no effect on the uterus and endometrium entity .
Estriol,Animal experiments have shown that estriol has a stronger effect on vaginal epithelial keratosis than estradiol , thus being able to promote vaginal epithelial hyperplasia , superficial cells keratosis , mucosal angiogenesis and vaginal epithelial wound healing , but having a weak effect on the weight gain of mouse uterus At the same time , estriol can enhance the function of cervix cell , causing the cervix muscle fiber hyperplasia and increasing the cervical elasticity and softness .
In addition , estriol has feedback inhibition on the hypothalamus and pituitary but does not inhibit ovulation while only having significant impact on the corpus luteum and therefore can be used as the auxiliary drug in the medium-term labor induction and artificial abortion and for the treatment of various kinds of menopathy . Estriol also has significant effect on the hematopoietic system and can reduce vascular permeability and fragility. Therefore , it can be used for the treatment of various kinds of hemorrhage . It also has effect of rapidly increasing the peripheral leukocytes and generally begins to take effect at 1 to 3 days after treatment but with a shorter duration of action and is effective in treatment the leukopenia induced by radiotherapy and chemotherapy .
|Melting Point||280-282 °C(lit.)|
|Boiling Point||469 °C at 760 mmHg|
|Flash Point||220.8 °C|
|Appearance||White crystalline powder|
|Package||as per request|
|Storage||as per relevent regulations|
Indications It can be used for treating cervicitis, especially suitable for treating menopausal syndrome and senile vaginitis. It can also be used as the adjuvant drug for middle-term labor induction and artificial abortion. It can also be used for treating prostatic hypertrophy and prostate cancer. In addition, it still has a rapid role in increasing the peripheral leukocytes. It generally takes effect at 1 to 3 days after the treatment but with a short duration period. It also has efficacy in treating leukopenia caused by chemotherapy or radiotherapy as well as reducing the vascular permeability and fragility and can be used for the treatment of various kinds of hemorrhage. It also has quick hemostasis effect on menorrhagia, hysterectomy or tonsillectomy.
|Description||Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.|
|In vitro||MTT assays using G-1 shows that, in SkBr3 cells, the proliferative effect induced by 100 nM G-1 is abolished in the presence of 1 μM estriol which acts as an antagonist of GPR30-dependent pathway. A cell-free transcription assay demonstrates that the antiestrogenic activity exhibited by estriol is because of interferring with estradiol-induced positive cooperative binding and receptor dimerization, binding of hER complexes to ERE, as well as reducing estradiol-dependent transcription in a dose-dependent manner. A recent study shows that estrogen (estrone, estradiol, and estriol) inhibits Alzheimer's disease-associated low-order Aβ oligomer formation, and among them, estriol shows the strongest in vitro activity.|
|In vivo||In mPTEN+/- mice, estriol treatments resulted in a 187.54% gain in the relative ratio of uterine wet weight to body weight; estriol also increases the ratio to 176.88% in wild-type mice. Estriol treatment (20 mg/kg ip), in vivo, sensitizes Kupffer cells to LPS via mechanisms dependent on an increase in CD14 by elevated portal blood endotoxin caused by increased gut permeability in rats; while one-half of the rats given estriol intraperitoneally 24 hours before an injection of a sublethal dose of LPS (5 mg/kg) died within 24 hours.
Purpose and Function
1. It can be used for treating cervicitis and especially suitable for treating menopausal syndrome and senile vaginitis.
2. It can also be used as the adjuvant drug for middle-term labor induction and artificial abortion.
3. It can also be used for treating prostatic hypertrophy and prostate cancer.
4. It still has a rapid role in increasing the peripheral leukocytes. It generally takes effect at 1 to 3 days after the treatment but with a short duration period. It also has efficacy in treating leukopenia caused by chemotherapy or radiotherapy.
5. It can be used for reducing the vascular permeability and fragility and can be used for the treatment of various kinds of hemorrhage. It also has quick hemostasis effect on menorrhagia, hysterectomy or tonsillectomy.
Chemical Properties It is white crystalline powder with the M.p. being 283 ºC, relative density being 1.27, and the specific rotation being [α] 25D + 34.4°(pyridine) and 25D + 58°± 5°(4%, dioxane). Its ethanol solution has maximum absorption at the wavelength of 280 nm. The crystal is insoluble in water, slightly soluble in ethanol (1: 500), diethyl ether, chloroform, dioxane and vegetable oil and easily soluble in pyridine and alkali hydroxide solution.
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