Date published: 2025-10-20

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Estradiol Inhibitors

Estradiol inhibitors are a class of chemical compounds designed to interfere with the biological activity of estradiol, a form of estrogen that plays a critical role in various physiological processes such as reproductive function, cell growth, and gene expression. Estradiol is synthesized from cholesterol through a series of enzymatic steps, primarily involving the enzyme aromatase, which converts androgens into estrogens. Inhibitors of estradiol can function by targeting different points along this biosynthetic pathway or by directly interacting with estrogen receptors. By inhibiting estradiol production or blocking its binding to receptors, researchers are able to study the regulatory mechanisms of estrogen signaling and its downstream effects on various cellular functions.

The chemical structures of estradiol inhibitors vary depending on their mechanism of action. Aromatase inhibitors, for instance, are designed to fit into the enzyme's active site, preventing the conversion of androgens to estradiol. These inhibitors often contain structural motifs that resemble the substrate of the enzyme, allowing for competitive inhibition. Other estradiol inhibitors, such as those that target estrogen receptors, are designed to mimic or block the natural ligand's binding, altering receptor conformation and preventing receptor-mediated gene transcription. Estradiol inhibitors are valuable tools in molecular biology for dissecting the roles of estrogen in gene regulation, cellular growth, and metabolic processes. Their use in research helps clarify the complex interactions between hormones and cellular signaling pathways, providing insights into how hormone levels regulate physiological and biochemical functions across various biological systems.

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Items 1 to 10 of 11 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Clomiphene Citrate

50-41-9sc-205636
sc-205636A
1 g
5 g
$82.00
$173.00
1
(0)

Clomiphene citrate functions by occupying estrogen receptors in the hypothalamus, leading to a decrease in the normal estrogen signaling required for estradiol production.

Tamoxifen

10540-29-1sc-208414
2.5 g
$256.00
18
(2)

Tamoxifen competes with estradiol for estrogen receptor binding, which can reduce the expression of genes involved in estradiol synthesis.

Raloxifene

84449-90-1sc-476458
1 g
$802.00
3
(0)

Raloxifene binds to estrogen receptors and can decrease the expression of estradiol by reducing estrogenic stimulation of the hypothalamic-pituitary axis.

Diethylstilbestrol

56-53-1sc-204720
sc-204720A
sc-204720B
sc-204720C
sc-204720D
1 g
5 g
25 g
50 g
100 g
$70.00
$281.00
$536.00
$1076.00
$2142.00
3
(1)

Diethylstilbestrol can exert a negative feedback on the hypothalamus and pituitary gland, which may lead to a reduced secretion of gonadotropins and subsequent decrease in ovarian estradiol synthesis.

Gossypol

303-45-7sc-200501
sc-200501A
25 mg
100 mg
$114.00
$225.00
12
(1)

Gossypol has the capability to interfere with the enzymatic activity in the steroidogenesis pathway, which can lead to a decrease in the synthesis of estradiol.

Danazol

17230-88-5sc-203021
sc-203021A
100 mg
250 mg
$90.00
$233.00
3
(0)

Danazol can suppress the secretion of gonadotropins from the pituitary gland, which can result in a decreased stimulation of ovarian follicles and reduced estradiol synthesis.

Mifepristone

84371-65-3sc-203134
100 mg
$60.00
17
(1)

Mifepristone, by antagonizing progesterone receptors, can lead to alterations in gonadotropin levels, which might subsequently decrease estradiol synthesis in the ovaries.

Letrozole

112809-51-5sc-204791
sc-204791A
25 mg
50 mg
$85.00
$144.00
5
(1)

Letrozole specifically inhibits the aromatase enzyme, leading to a significant decrease in the conversion of androgens to estradiol in peripheral tissues.

Trilostane

13647-35-3sc-208469
sc-208469A
10 mg
100 mg
$224.00
$1193.00
2
(1)

Trilostane directly inhibits the enzyme 3β-hydroxysteroid dehydrogenase, which is crucial for the biosynthesis of estradiol, resulting in decreased estradiol levels.

Finasteride

98319-26-7sc-203954
50 mg
$103.00
3
(1)

Finasteride reduces the production of dihydrotestosterone without directly decreasing estradiol levels, but the altered androgen to estrogen ratio can indirectly downregulate the body's estradiol synthesis.