17β-HSD Activators
HSD17B1 activators comprise a chemical class that influences the enzymatic activity of HSD17B1, primarily by modulating substrate availability or through feedback mechanisms. These activators encompass both endogenous substrates and exogenous compounds that either serve directly as substrates for the enzyme's catalytic action or enhance substrate levels through the inhibition of competing pathways. The primary endogenous substrates include androgenic steroids like androstenedione and DHEA, which HSD17B1 converts to more potent androgens and estrogens, a core step in steroidogenesis. The presence of these substrates can enhance the activity of HSD17B1 by providing the necessary molecules for its action.
Furthermore, the inhibition of aromatase by compounds such as letrozole, and exemestane contributes to an increase in androgen levels. Since aromatase is responsible for the conversion of androgens to estrogens, these inhibitors prevent the depletion of androgens, thus indirectly promoting the action of HSD17B1 by ensuring an ample supply of its substrates. On the other hand, estradiol itself, through a positive feedback loop, can enhance HSD17B1 activity by increasing the enzyme's substrate availability, showcasing a dynamic interplay where the product of the reaction further stimulates the enzymatic process.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
β-Estradiol | 50-28-2 | sc-204431 sc-204431A | 500 mg 5 g | $63.00 $182.00 | 8 | |
Estradiol directly increases HSD17B1 activity by enhancing its substrate availability, as HSD17B1 is responsible for converting estrone to the more active estrogen, estradiol. Increased levels of estradiol can create a positive feedback loop, further stimulating HSD17B1 activity. | ||||||
Fadrozole hydrochloride | 102676-31-3 | sc-252819 sc-252819A sc-252819B | 10 mg 50 mg 500 mg | $141.00 $541.00 $4162.00 | ||
Fadrozole, an aromatase inhibitor, elevates the levels of androgens which are substrates for HSD17B1. By inhibiting the conversion of androgens to estrogens, fadrozole can indirectly increase HSD17B1 activity by ensuring more substrate availability for the conversion of weaker androgens to stronger ones. | ||||||
Exemestane | 107868-30-4 | sc-203045 sc-203045A | 25 mg 100 mg | $134.00 $411.00 | ||
Exemestane is another aromatase inhibitor that leads to increased availability of androgens for HSD17B1 to act upon. This boosts the enzymatic activity of HSD17B1 by providing more substrate for the conversion processes that it mediates. | ||||||
Letrozole | 112809-51-5 | sc-204791 sc-204791A | 25 mg 50 mg | $87.00 $147.00 | 5 | |
Letrozole acts by inhibiting the aromatase enzyme, leading to an increased concentration of androgens. This abundance can promote the enzymatic activity of HSD17B1 as it converts these androgens into estrogens, indicating an indirect activation of HSD17B1's role in steroidogenesis. | ||||||
Chrysin | 480-40-0 | sc-204686 | 1 g | $38.00 | 13 | |
Chrysin is a naturally occurring flavonoid that exhibits aromatase-inhibiting properties. This inhibition can lead to higher levels of androgens, providing more substrates for HSD17B1 and thereby potentially upregulating the activity of HSD17B1. | ||||||
DHEA | 53-43-0 | sc-202573 | 10 g | $111.00 | 3 | |
DHEA serves as a substrate for HSD17B1 in the biosynthesis of androgens and estrogens. Elevating DHEA levels can, therefore, enhance HSD17B1 activity by providing more substrate for conversion, which is an essential step in steroid hormone production. | ||||||
Progesterone | 57-83-0 | sc-296138A sc-296138 sc-296138B | 1 g 5 g 50 g | $20.00 $52.00 $298.00 | 3 | |
Progesterone can be metabolized by HSD17B1 to androgens and subsequently to estrogens. Increasing progesterone levels can lead to upregulated activity of HSD17B1 as it processes more substrate through the steroidogenesis pathway. | ||||||