Enclomifene (INNTooltip International Nonproprietary Name), or enclomiphene (USANTooltip United States Adopted Name), a nonsteroidal selective estrogen receptor modulator of the triphenylethylene group acts by antagonizing the estrogen receptor (ER) in the pituitary gland, which reduces negative feedback by estrogen on the hypothalamic-pituitary-gonadal axis, thereby increasing gonadotropin secretion and hence gonadal production of testosterone. It is one of the two stereoisomers of clomifene, which itself is a mixture of 38% zuclomifene and 62% enclomifene. Enclomifene is the (E)-stereoisomer of clomifene, while zuclomifene is the (Z)-stereoisomer. Whereas zuclomifene is more estrogenic, enclomifene is more antiestrogenic. In accordance, unlike enclomifene, zuclomifene is antigonadotropic due to activation of the ER and reduces testosterone levels in men. As such, isomerically pure enclomifene is more favorable than clomifene as a progonadotropin for the treatment of male hypogonadism.
enclomiphene before and after
Enclomiphene (former tentative brand names Androxal and EnCyzix), was under development for the treatment of male hypogonadism and type 2 diabetes. By December 2016, it was in preregistration and was under review by the Food and Drug Administration in the United States and the European Medicines Agency in the European Union. In January 2018, the Committee for Medicinal Products for Human Use of the European Medicines Agency recommended refusal of marketing authorization for enclomifene for the treatment of secondary hypogonadism. In April 2021, development of enclomifene was discontinued for all indications.
The key difference between encl citrate and traditional testosterone replacement therapy is that enclomiphene citrate stimulates the body to produce its own testosterone, while traditional testosterone replacement therapy replaces low testosterone levels in men with exogenous, synthetic testosterone.
Description
Sarm Enclomiphene is a synthetic and nonsteroidal antiestrogen. It is the more potent isomer and the one responsible for its ovulation-inducing actions. The half-life of enclomiphene is relatively short, so serum concentrations rise and fall quickly during and after treatment. Antiestrogens represent the first-line treatment strategy in WHO class-2 anovulatory infertility.
Uses trans-Clomiphene is a Clomiphene (C587025) stereoisomer, a synthetic estrogen agonist-antagonist. Gonad-stimulating principle. Treatment for infertility.
Definition ChEBI: Clomiphene is a tertiary amine. It has a role as an estrogen antagonist and an estrogen receptor modulator. It derives from a hydride of a stilbene.
Preparation CONDENSATION OF 4-HYDROXYBENZOPHENONE WITH 2-(DIETHYLAMINO)ETHYL CHLORIDE FOLLOWED BY TREATMENT WITH BENZYL MAGNESIUM CHLORIDE AND DEHYDRATION TO GIVE 2-(P-(1,2-DIPHENYLVINYL)PHENOXY)TRIETHYLAMINE WHICH IS CHLORINATED AND TREATED WITH CITRIC ACID /CITRATE/
Biological Activity
Enclomiphene pct dosage is the trans-isomer of clomiphene citrate (CC). It has a higher rate of clearance and is less active than the cis-isomer, cis-clomiphene. Clomiphene citrate has been evaluated for antineoplastic activity against breast cancer.
Mode of action Encl is a non-steroidal estrogen receptor antagonist that promotes gonadotropin-dependent testosterone secretion by the testes. The main mechanism of its action is thought to be its antagonistic effects on the hypothalamic-pituitary axis and stimulation of GnRH secretion.
Enclomiphene powder Chemical Properties
Melting point 149.0-150.5°
Boiling point 509.0±50.0 °C(Predicted)
density 1.104±0.06 g/cm3(Predicted)
pka 9.60±0.25(Predicted)
More Introduction:https://en.wikipedia.org/wiki/Enclomifene
