17β-estradiol

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 (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).

beta-Estradiol 17-hemisuccinate selectively stains estrogen receptor (ER)-rich cells.

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-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.

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.

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.

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-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.

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.

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.

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.

6-Ketoestradiol, an active metabolite of the endogenous estrogen estrone [1].

β-Estradiol 17-acetate (1,3,5(10)-Estratriene-3,17β-diol 17-acetate) is a metabolite of estradiol.

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.

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.

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

HSD17B13-IN-58 (96) acts as an inhibitor of 17β-Hydroxysteroid dehydrogenases (HSD17B13), demonstrating potent activity with an IC 50 of less than 0.1 μM for Estradiol. This compound is primarily utilized in research related to Nonalcoholic fatty liver diseases (NAFLD) [1].

Compound 16 (HSD17B13-IN-68) acts as an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting potent activity with an IC50 value of less than 0.1 μM against estradiol. It facilitates research into liver diseases or metabolic disorders [1].

HSD17B13-IN-71 (Compound 149), an effective inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), displays potent activity with an IC 50 value of ≤ 0.1 μM against estradiol. This compound is applicable in the study of various disorders including liver diseases, metabolic diseases, and cardiovascular conditions such as NAFLD or NASH, in addition to drug-induced liver injury (DILI) [1].

HSD17B13-IN-84 (182) serves as an inhibitor of 17β-Hydroxysteroid dehydrogenases (HSD17B13), exhibiting an IC50 of less than 0.1 μM for Estradiol. It is primarily utilized in the study of NAFLD (Nonalcoholic fatty liver diseases) [1].

HSD17B13-IN-89 (206) acts as an inhibitor of 17β-Hydroxysteroid dehydrogenases (HSD17B13) and demonstrates potent activity with an IC 50 value of less than 0.1 μM for Estradiol. It is commonly utilized in research related to Nonalcoholic Fatty Liver Diseases (NAFLD) [1].

HSD17B13-IN-95 (1) serves as an inhibitor for 17 β-hydroxysteroid dehydrogenase (HSD17B13), exhibiting an IC50 value of <0.1 μM for estradiol. It is applicable in researching nonalcoholic fatty liver disease [1].

HSD17B13-IN-12 (Compound 3), functioning as an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibits potent activity with an IC 50 value of ≤ 0.1 μM against both leukotriene B3 and estradiol. This compound is applicable in studying various conditions including liver diseases, metabolic disorders, and cardiovascular diseases like NAFLD or NASH, as well as drug-induced liver injury (DILI) [1].

HSD17B13-IN-17 (compound 9) serves as a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13). It demonstrates inhibitory efficacy with IC50 values of ＜0.1 μM for estradiol and ＜1 μM for Leukotriene B3 as substrates. This compound is significant in the management of nonalcoholic fatty liver diseases (NAFLDs), including nonalcoholic steatohepatitis (NASH) [1].

HSD17B13-IN-52 (Compound 84), an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibits potent activity with an IC50 value of ≤ 0.1 μM against estradiol. This compound is applicable in the research of various health conditions including liver, metabolic, and cardiovascular diseases, specifically NAFLD, NASH, and drug-induced liver injury (DILI) [1].

HSD17B13-IN-55 (Compound 167) serves as an effective inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting an IC 50 value of ≤ 0.1 μM against estradiol. This compound is particularly useful in research related to liver, metabolic, and cardiovascular diseases including NAFLD, NASH, and drug-induced liver injury (DILI) [1].

HSD17B13-IN-57 (Compound 93) acts as an inhibitor targeting hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), demonstrating an IC 50 of ≤ 0.1 μM against estradiol. This compound is applicable in the study of various health conditions, including liver, metabolic, and cardiovascular diseases—specifically NAFLD, NASH—and drug-induced liver injury (DILI) [1].

HSD17B13-IN-19 (compound 16) acts as a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting IC50 values under 0.1 μM and under 1 μM when using estradiol and Leukotriene B3 as substrates, respectively. This compound is crucial in the treatment of nonalcoholic fatty liver diseases (NAFLDs), such as nonalcoholic steatohepatitis (NASH) [1].

HSD17B13-IN-28 (compound 47) is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), with an IC50 of < 0.1 μM using estradiol as a substrate. HSD17B13-IN-28 plays an important role in nonalcoholic fatty liver diseases (NAFLDs), including NASH (nonalcoholic steatohepatitis) [1].

HSD17B13-IN-32 (Compound 67) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC50 value of ≤0.1 μM for estradiol. It can be used for research on liver diseases, metabolic diseases, or cardiovascular diseases, such as NAFLD or NASH, as well as drug-induced liver injury (DILI) [1].

HSD17B13-IN-40 (compound 6) serves as a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting an IC50 value of less than 0.1 μM using estradiol as substrates. This compound is significant in the treatment of nonalcoholic fatty liver diseases (NAFLDs), including nonalcoholic steatohepatitis (NASH) [1].

HSD17B13-IN-42 (compound 10) is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), with an IC50 of < 0.1 μM using estradiol as substrates. HSD17B13-IN-42 plays an important role in nonalcoholic fatty liver diseases (NAFLDs) including NASH (nonalcoholic steatohepatitis) [1].

HSD17B13-IN-44 (Compound 23) functions as an inhibitor targeting hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting an IC50 value of < 0.1 μM against estradiol. This compound is applicable in the study of liver diseases or metabolic disorders [1].

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].

HSD17B13-IN-13 (Compound 5), an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), demonstrates potent activity with an IC 50 value of less than 0.1 μM against estradiol. This compound is applicable in the study of liver diseases, including NAFLD [1].

HSD17B13-IN-15 (Compound 6) acts as an inhibitor targeting hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting IC 50 values of ≤ 1 μM for leukotriene B3 and ≤ 0.1 μM for estradiol. This compound finds applications in studying various conditions, including liver diseases, metabolic disorders, and cardiovascular diseases such as NAFLD, NASH, or drug-induced liver injury (DILI) [1].

HSD17B13-IN-47 (Compound 500), an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), demonstrates potent activity with an IC 50 value of < 0.1 μM against estradiol. It is applicable in the study of liver diseases or metabolic disorders [1].

HSD17B13-IN-51 (Compound 82), an inhibitor targeting hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibits potent activity with an IC50 value of ≤ 0.1 μM against estradiol. This compound is useful in researching various conditions including liver, metabolic, and cardiovascular diseases—specifically NAFLD, NASH, and drug-induced liver injury (DILI) [1].

HSD17B13-IN-53 (Compound 88) serves as an inhibitor targeting hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), demonstrating an IC 50 of ≤ 0.1 μM against estradiol. This compound is utilized in the study of liver, metabolic, and cardiovascular diseases, including NAFLD and NASH, besides its application in drug-induced liver injury (DILI) [1].

HSD17B13-IN-54 (Compound 158) functions as an inhibitor targeting hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting an IC 50 value of ≤ 0.1 μM against estradiol. This compound holds potential for applications in the study of various liver, metabolic, and cardiovascular diseases, including NAFLD and NASH, as well as drug-induced liver injury (DILI) [1].

HSD17B13-IN-64 (Compound 143), an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibits a potent IC50 value of ≤ 0.1 μM against estradiol. This compound has applications in the study of various diseases, including liver conditions like NAFLD and NASH, metabolic and cardiovascular disorders, as well as drug-induced liver injury (DILI) [1].

Compound 677 (HSD17B13-IN-67) acts as an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting an IC 50 value of < 0.1 μM for estradiol. It has potential applications in research focused on liver diseases or metabolic disorders [1].

HSD17B13-IN-72 (Compound 62), an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibits potent activity with an IC 50 value of < 0.1 μM for estradiol. This compound is utilized in the study of liver diseases or metabolic disorders [1].

HSD17B13-IN-24 (41) acts as an inhibitor of 17β-Hydroxysteroid dehydrogenases (HSD17B13), exhibiting a potent IC50 value of <0.1 μM for Estradiol. It is primarily utilized in the study of NAFLD (Nonalcoholic fatty liver diseases) [1].

HSD17B13-IN-43 (11) serves as an inhibitor of 17β-Hydroxysteroid dehydrogenases (HSD17B13), demonstrating potent activity with an IC 50 of <0.1 μM against Estradiol. It is primarily utilized in the study of NAFLD (Nonalcoholic fatty liver diseases) [1].

HSD17B13-IN-79 (Compound 32), an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), demonstrates potent activity with an IC50 value of ≤ 0.1 μM against estradiol. This compound is primarily utilized in the study of liver, metabolic, and cardiovascular diseases, including non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and drug-induced liver injury (DILI) [1].