Estrogen Steroids Estradiol Benzoate Valerate

Estrogen Steroids Estradiol Benzoate CAS 50-50-0 Oestradiol Benzoate With high quality and best pric e Estradiol Valerate Estradiol Benzoate Quick Details: CAS No.:50-50-0 Other Names:17beta-Estradiol benzoate MF:C25H28O3 EINECS...
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Estrogen Steroids Estradiol Benzoate CAS 50-50-0 Oestradiol Benzoate With high quality and best price Estradiol Valerate


Estradiol Benzoate 

Quick Details:

CAS No.:50-50-0

Other Names:17beta-Estradiol benzoate

MF:C25H28O3

EINECS No.:200-043-7

Place of Origin:ShenZhen, China (Mainland)

Type:Auxiliaries and Other Medicinal Chemicals

Grade Standard:Medicine Grade, Tech Grade

Brand Name:SENDI

Model Number:--

Purity:99% Min

Name:Estradiol Benzoate

Packing:1kg/bag

apperance:White powder

Usage: Ethynylestradiol is a derivative of estradiol. Ethynyl estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills (the Pill). It is one of the most commonly used medications.Estinyl was a preparation of EE alone that was used for the management of menopausal symptoms and female hypogonadism.

Ethynyl Estradiol is a synthetic analog of estradiol, often used in combination with a progestin. Efficacy of administration is facilitated by the ethynyl substitution at the C-17 position, which inhibits first pass hepatic metabolism. Rapidly absorbed from gastrointestinal tract.Usage:Ethynyl estradiol ,A synthetic steroid with high oral estrogenic potency

Function:
 
Supplement estrogen therapy adverse female gonadal function, amenorrhea, menopausal syndrome; for advanced breast cancer (in postmenopausal women), advanced prostate cancer treatment; in combination with progestin drugs, can inhibit ovulation, can be used contraceptives. The main clinical drug used to inhibit ovulation; also used in pediatric cryptorchidism and androgen excess, pituitary tumors. For the diagnosis of hypothalamic - pituitary - gonadal dysfunction, which can be carried out in accordance with gonadotropin and sex hormone levels.

Treatment of hypogonadotropic hypogonadism due to amenorrhea and infertility, polycystic ovarian infertility. Amenorrhea associated with weight loss, you should use correct diet weight. Also for prostate cancer (often in combination with cyproterone or fluoro methyl imide), delayed puberty or early endometrial bit different. Used primarily for inhibiting ovulation to achieve the purpose of contraception.


What is Estradiol Benzoate ?
White or light yellow crystalline powder.Odourless.Tasteless.Stability in the air.Melting_point191-196℃.A dextral light.Soluble in ethanol, acetone, 4-dioxane o 2, slightly soluble in vegetable oils, soluble in ether, almost insoluble in water.

1. Hypoplasia of uterus after less, amenorrhea, or month

2. Menopausal syndrome women entered a period years, ovarian function decline gradually

3. Breast pain (milk) back stop lactating breast tenderness, with large dose of estrogen that can eliminate

4. Prostate cancer

5. Postmenopausal osteoporosis and senile osteoporosis using estrogen therapy, can reduce the bone absorption, prevent the fracture.

6. Men and women of acne (pimples), see more at puberty, is androgen stimulates the sebaceous glands

7. contraception

COA
 

ItemSpecificationResults
AppearanceWhite to creamy white, odorless, crystalline powder.white crystalline powder
SolubilityInsoluble in water; soluble in alcohol, in chloroform, in ether, in vegetable oils, and in solutions of fixed alkali hydroxides.Conforms
IdentificationA:IR B:UVConforms
Specific optical rotation-28°~ -29.5°-28.3°
Melting range180~186ºC182.5~185.3ºC
Loss on drying≤1.0%0.45%
Residual SolventsAcetone≤0.5%0.08%
Assay97.0~102.0% (on the dried basis)99.9%
Particle Size90% ≤10μConforms
ConclusionThe product complies with specification in USP34

Estradiol benzoate, sold under the brand name Progynon-B among others, is a medication which is used in hormone therapy such as for menopausal symptoms and in veterinary medicine. It is given by injection into muscle.


Side effects of estradiol benzoate include breast tenderness, breast enlargement, nausea, headache, and fluid retention.The drug is a synthetic estrogen and hence is an agonist of the estrogen receptor (ER), the biological target of estrogens like estradiol. Estradiol benzoate is an estrogen ester and a prodrug of estradiol in the body. Because of this, it is considered to be a natural and bioidentical form of estrogen.

Estradiol benzoate was discovered in 1933 and was introduced for medical use in 1936. It was the first estradiol ester to be discovered or marketed and was one of the first estrogens to be introduced for medical use. Along with estradiol dipropionate, it was among the most widely used esters of estradiol for many years after its introduction. However, in the 1950s, longer-acting estradiol esters that require less frequent injections like estradiol valerate and estradiol cypionate were developed and have since mostly superseded estradiol benzoate. In spite of this, estradiol benzoate remains widely available throughout the world. It is not available for medical use in the United States.

Medical uses

Main article: Estradiol (medication) § Medical uses

The medical uses of estradiol benzoate are the same as those of estradiol and other estrogens. An example of an indication for the drug is hormone therapy for menopausal symptoms or hypoestrogenism.

Side effects

Main article: Estradiol (medication) § Side effects

The side effects of estradiol benzoate are the same as those of estradiol. Examples of such side effects include breast tenderness and enlargement, nausea, bloating, edema, headache, and melasma.


Pharmacology

Pharmacodynamics

Esters of estradiol like estradiol benzoate are readily hydrolyzed prodrugs of estradiol, but have an extended duration when administered in oil via intramuscular injection due to a depot effect afforded by their fatty acid ester moiety. As prodrugs of estradiol, estradiol benzoate and other estradiol esters are estrogens, or agonists of the estrogen receptors (ERs).

Estradiol benzoate has very low affinity for the ERs, on the order of 100-fold less than that of estradiol. As such, estradiol benzoate is an inactive prodrug of estradiol.


Pharmacokinetics

Upon ingestion, regardless of the route of administration, estradiol benzoate behaves as a prodrug via cleavage by esterases into estradiol and the natural fatty acid benzoic acid. This cleavage occurs not only in the liver, but also in the blood and in tissues.


A single dose of 2.5 mg estradiol benzoate by intramuscular injection was found to produce plasma estradiol levels of >400 pg/mL, measured 24 hours post-injection, in a group of patients with minimal baseline levels of estradiol (due to GnRH analogue therapy with triptorelin).


Intramuscular administration:

A single intramuscular injection of 5 mg estradiol benzoate has been found to result in peak circulating concentrations of 940 pg/mL estradiol and 343 pg/mL estrone, which occurred at about 2 days post-injection (see table). Compared to two other commonly used estradiol esters (which were also assessed in the study), estradiol benzoate had the shortest duration, at approximately 4 to 5 days, whereas estradiol valerate and estradiol cypionate were found to last for 7–8 days and 11 days, respectively. This is because estradiol benzoate has a shorter and less bulky fatty acid chain and in relation to this is comparatively less lipophilic. For a given estradiol ester, the shorter or less extensive the fatty acid chain is, the less lipophilic, shorter-lasting, and less uniform/plateau-like the resultant levels of estradiol are as well as the higher the peak/maximal levels are (and hence more spike-like).

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