17β-Estradiol

17β-Estradiol sulfate sodium (17β-Estradiol 3-sulfate sodium) is a neuroactive estrogen with vasoprotective properties that inhibits the growth of Neisseria brasiliensis and disrupts aquatic ecosystems.

Estradiol 17-(β-D-glucuronide) (E217G) is an estrogen metabolite formed in the liver and subsequently excreted in bile.1It acts as a substrate of the multidrug resistance protein 2 (MRP2; Km= 75 μM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.1,2In addition to binding to the MRP2 transport site, E217G has been shown to bind to an allosteric site that through positive cooperativity activates its own transportviaMRP2 and the transport of other MRP2 substrates, including the non-cholestatic estrogen metabolite, estradiol 3-(β-D-glucuronide) .2,3E217G has also been reported to be transported by MDR1, MRP1, MRP3, MRP4, MRP7, ABCG2 (a breast cancer resistance protein transporter), and the rat organic anion-transporting polypeptides 1-4.2 1.Loe, D.W., Almquist, K.C., Cole, S.P., et al.ATP-dependent 17β-estradiol 17-(β-D-glucuronide) transport by multidrug resistance protein (MRP). Inhibition by cholestatic steroidsThe Journal of Biological Chemisty271(16)9683-9689(1996) 2.Gerk, P.M., Li, W., and Vore, M.Estradiol 3-glucuronide is transported by the multidrug resistance-associated protein 2 but does not activate the allosteric site bound by estradiol 17-glucuronideDrug Metabolism and Disposition32(10)1139-1145(2004) 3.Gerk, P.M., Li, W., Megaraj, W., et al.Human multidrug resistance protein 2 transports the therapeutic bile salt tauroursodeoxycholateJournal of Pharmacology and Experimental Therapeutics320(2)893-899(2007)

Estradiol 3-sulfate 17β-Glucuronide potassium salt (Estradiol 3-sulfate 17-glucuronide potassium) is a naturally occurring estrogen that competitively inhibits MRP-mediated LTC transporter and can be used to study metabolic diseases.

17β-estradiol-d4 is a deuterated compound of 17β-estradiol. 17β-estradiol has a CAS number of 50-28-2. Estradiol is an Estrogen. The mechanism of action of estradiol is as an Estrogen Receptor Agonist.

16α-Hydroxy-17β-estradiol-2,4-d2 is a deuterated compound of Estriol. Estriol has a CAS number of 50-27-1. Estriol is a hydroxylated metabolite of ESTRADIOL or ESTRONE that has a hydroxyl group at C3, 16-alpha, and 17-beta position. Estriol is a major urinary estrogen. During PREGNANCY, a large amount of estriol is produced by the PLACENTA.

17β-Estradiol-16,16,17-d3 is a deuterated compound of 17β-Estradiol. 17β-Estradiol has a CAS number of 50-28-2. Estradiol is an Estrogen. The mechanism of action of estradiol is as an Estrogen Receptor Agonist.

17β-Estradiol-16,16-d2 is a deuterated compound of 17β-Estradiol. 17β-Estradiol has a CAS number of 50-28-2. Estradiol is an Estrogen. The mechanism of action of estradiol is as an Estrogen Receptor Agonist.

4-Methoxy-17-estradiol is one of the estrogen metabolites and a methylation metabolite of 4-hydroxyestradiol.

17β-Estradiol-2,4,16,16,17-d5 is a deuterated compound of 17β-Estradiol. 17β-Estradiol has a CAS number of 50-28-2. Estradiol is an Estrogen. The mechanism of action of estradiol is as an Estrogen Receptor Agonist.

17β-Estradiol-2,4-d2 is a deuterated compound of 17β-Estradiol. 17β-Estradiol has a CAS number of 50-28-2. Estradiol is an Estrogen. The mechanism of action of estradiol is as an Estrogen Receptor Agonist.

17β-Estradiol-2,4-d2 (Standard) is the standard substance of 17β-Estradiol-2,4-d2, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. 17β-Estradiol-2,4-d2 is a deuterated compound of 17β-Estradiol. 17β-Estradiol has a CAS number of 50-28-2. Estradiol is an Estrogen. The mechanism of action of estradiol is as an Estrogen Receptor Agonist.

10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-selective prodrug of 17β-estradiol, which has neuroprotective effects, improves cognitive dysfunction, and can be used to study brain damage.

G36 is a cell-permeable non-steroidal antagonist of GPER. G36 inhibits activation by either 17β-estradiol or the GPER-selective agonist G-1 (IC50 = 112 and 165 nM, respectively). G36 has no detectable binding activity to either ERα or ERβ. G36 blocks the activation of PI3K or calcium mobilization triggered by estrogen through GPER and it suppresses ERK activation by estrogen or G-1 but not by EGF. G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ERα and ERβ in complex biological systems.

Estradiol cypionate (Depofemin), the 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptor.

Estradiol (E2) is a naturally occurring steroidal sex hormone that is essential for female fertility and maintenance of secondary sexual characteristics. Estradiol upregulates IL-6 expression through estrogen receptor beta (ERβ).

17β-HSD7-IN-1 (compound 4) acts as an inhibitor of 17β-HSD7, effectively suppressing the formation of estradiol with an IC50 value of 63 nM.

(E/Z)-Droloxifene is a mixture comprising (E)-Droloxifene, known as a selective estrogen receptor modulator, and (Z)-Droloxifene. (E)-Droloxifene binds to estrogen receptors (ER) in rabbit uterine homogenate with an IC50 of 24 nM. It increases uterine weight in immature rats and reduces the uterine weight increase caused by estradiol in juvenile rats. Additionally, (E)-Droloxifene inhibits the growth of human breast cancer cells MCF-7, ZR-75-1, and T47D stimulated by 17β-estradiol. In contrast, (Z)-Droloxifene shows weak binding to ER and exhibits neither estrogenic nor anti-estrogenic activity.

3-O-methyl Estradiol is a synthetic estrogen known for its ability to interfere with microtubule networks in V79 Chinese hamster cells, with an EC50 value of 9 µM. At a concentration of 20 µM, it inhibits the proliferation of these cells by 92%. Additionally, when male rats on a high-cholesterol diet are administered 3-O-methyl Estradiol (25 mg in a 0.2 ml solution, p.o.), it results in decreased serum cholesterol levels and increases body weight loss, suggesting feminizing effects. It has also been utilized as a standard for quantifying 17β-estradiol in hen urine.

HSD17B13-IN-4 (Compound 95) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with a Ki value for the substrate estradiol LCMS of ≤ 50 nM. It can be utilized in research on liver diseases, metabolic disorders, or cardiovascular diseases such as NAFLD, NASH, or drug-induced liver injury (DILI).

HSD17B13-IN-5 (Compound 96) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with a Ki value of ≤ 50 nM for the estradiol substrate LCMS. It is applicable in research on liver diseases, metabolic disorders, or cardiovascular conditions, such as NAFLD or NASH, or drug-induced liver injury (DILI).

HSD17B13-IN-101 is a selective inhibitor of 17β-hydroxysteroid dehydrogenase (HSD17B13), exhibiting an IC50 value of less than 0.1 μM for estradiol. It is applicable in research on non-alcoholic fatty liver disease (WO2023146897A1; compound 94).

17-Epiestriol is a metabolite of estrone .1It is formed from estroneviaa 16α-hydroxy estrone intermediate by reduction of the C-17 ketone. 17-Epiestriol binds to estrogen receptor α (ERα) and ERβ with relative binding affinities of 29 and 80 compared with 17β-estradiol .2 1.Brinton, L.A., Trabert, B., Anderson, G.L., et al.Serum estrogens and estrogen metabolites and endometrial cancer risk among postmenopausal womenCancer Epidemiol. Biomarkers Prev.25(7)1081-1089(2016) 2.Kuiper, G.G.J.M., Lemmen, J.G., Carlsson, B., et al.Interaction of estrogenic chemicals and phytoestrogens with estrogen receptor βEndocrinology139(10)4252-4263(1998)

TPBM is a potent inhibitor of estrogen receptor α (ERα). The IC 50 value of TPBM for 17β-estradiol (E2)-ERα is 9 μM. TPBM is not toxic to cells and reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells with an IC 50 value of 5 μM. TPBM does not affect estrogen-independent cell growth [1].

Estradiol (β-Estradiol) hemihydrate, a key female sex hormone and steroid, plays a significant role in up-regulating neural markers in human endometrial stem cells (hEnSCs) and facilitating their neural differentiation. It is also utilized in research focused on cancers, neurodegenerative diseases, and neural tissue engineering.