Home Metabolism Endogenous Metabolite inhibitor 17β-Estradiol

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17β-Estradiol Human Endogenous Metabolite

Cat.No.S1709

Estradiol (17β-estradiol, β-Estradiol, E2, 17β-Oestradiol) is a human sex hormone and steroid, and the primary female sex hormone. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
17β-Estradiol Endogenous Metabolite inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 272.38

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Quality Control

Batch: Purity: 99.99%
99.99

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 Function assay Displacement of [3H]estradiol from Estrogen receptor in MCF-7 cells, IC50=0.003μM 1548683
MCF-7 Function assay Effective dose for [3H]- estradiol against proliferation of MCF-7 cells, EC50=0.00002μM 2769681
Ishikawa cells Function assay Concentration of compound required to induce 50 % of the maximum stimulation of alkaline phosphatase activity in Ishikawa cells, EC50=0.00001μM 8201587
MCF-7 Function assay Induction of pS2 mRNA expression in human MCF-7 mammary carcinoma cells, EC50=0.0000996μM 8627615
MCF-7 Function assay Induction of pS2 mRNA expression in human MCF-7 mammary carcinoma cells, EC50=0.000292μM 8627615
mammary cancer cells Function assay Affinity estrogen receptor of MCF-7 human mammary cancer cells, EC50=0.0038μM 8627615
HeLa Function assay TP_TRANSPORTER: inhibition of E217betaG uptake in Oatp1-expressing HeLa cells, Ki=4.7μM 8779894
MCF-7 Function assay Growth response in cultures of MCF-7 (human breast cancer cell line) cells, EC50=0.0000015μM 9357533
MCF-7 Function assay Induction of pS2 Gene expression in human MCF-7 cells, EC50=0.0000301μM 9371241
MCF-7 Function assay Affinity for estrogen receptor of human MCF-7 cells, EC50=0.00018μM 9371241
HRPE Function assay TP_TRANSPORTER: inhibition of TEA uptake (TEA: 20 uM) in OCT3-expressing HRPE cells, IC50=1.1μM 9830022
MCF-7 Function assay Agonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alpha, EC50=0.000007μM 10673099
HeLa Function assay Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor alpha., EC50=0.00002μM 11906280
HeLa Function assay Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor beta., EC50=0.00007μM 11906280
SH-SY5Y Function assay Agonist activity in transcriptional activation assay in SH-SY5Y neuroblastoma cells expressing Estrogen receptor beta, EC50=0.0001μM 11906280
HEK293 Function assay TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT3-expressing HEK293 cells, IC50=2.88μM 12110607
HEK293 Function assay TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT1-expressing HEK293 cells, IC50=5.73μM 12110607
MCF-7-2a Function assay Agonist activity in transcriptional activation assay in MCF-7-2a cells compared to estradiol E2, EC50=0.00049μM 12139447
T47D Function assay Agonist effect on transcriptional activation in T47D cells expressing estrogen receptor alpha, EC50=0.00007μM 12459017
T47D Function assay Agonist effect on transcriptional activation of T47D cells expressing human estrogen receptor beta, EC50=0.0008μM 12459017
MCF-7 Function assay Percent agonistic activity for estrogen-induced pS2 expression in MCF-7 cells, EC50=0.00001μM 12749898
MCF-7 Function assay Functional ERalpha receptor activity in transcriptional activation assay in MCF-7 cells, ED50=0.0000046μM 12824043
SAOS-2 Function assay Functional Estrogen receptor beta activity by metallothionein induction in SAOS-2 cells, ED50=0.0047μM 12824043
MCF-7 breast tumor Function assay Effective concentration against MCF-7 breast tumor cells using MCF-7 assay., EC50=0.00001μM 12825935
MCF-7-2a Function assay Concentration required to activate luciferase expression in MCF-7-2a cells, EC50=0.00008μM 14761193
Ishikawa Var-1 cells Function assay 72 hrs Estrogenic activity at estrogen receptor in human Ishikawa Var-1 cells assessed as stimulation of alkaline phosphatase activity measured by metabolism of p-nitrophenol phosphatase after 72 hrs, EC50=0.000047μM 15568770
HeLa Function assay Inhibition of [3H]estradiol binding to human estrogen receptor beta expressed in HeLa cells, IC50=0.024μM 15658851
HeLa Function assay Inhibition of [3H]estradiol binding to human estrogen receptor alpha expressed in HeLa cells, IC50=0.028μM 15658851
COS-1 Function assay In vitro agonist activity for estrogen receptor alpha expressed in COS-1 cells, EC50=0.0024μM 15713407
COS-1 Function assay In vitro agonist activity for estrogen receptor beta expressed in COS-1 cells, EC50=0.0097μM 15713407
293T Function assay Displacement of [3H]17beta-estradiol from recombinant human ERalpha expressed in 293T cells, IC50=0.00075μM 16219463
293T Function assay Displacement of [3H]17beta-estradiol from recombinant human ERbeta expressed in 293T cells, IC50=0.00118μM 16219463
HEK293 Function assay Effect on transactivation of ALP gene expression in HEK293 cells transfected with hERalpha, EC50=0.00075μM 16309907
HEK293 Function assay Effect on transactivation of ALP gene expression in HEK293 cells transfected with hERbeta, EC50=0.0021μM 16309907
SK-BR-3 Function assay 48 hrs Inhibition of chemoattractant-induced cell migration of human SK-BR-3 cells after 48 hrs by transwell migration assay, IC50=0.0001μM 16520733
COS7 Function assay Displacement of E2-Alexa633 from GFP-tagged ERalpha expressed in COS7 cells by FACS, Ki=0.0003μM 16520733
COS7 Function assay Agonist activity at GFP-tagged GPR30 expressed in COS7 cells assessed as half life for increase in intracellular calcium level by spectrofluorimetry, EC50=0.0003μM 16520733
COS7 Function assay Displacement of E2-Alexa633 from GFP-tagged ERbeta expressed in COS7 cells by FACS, Ki=0.00038μM 16520733
MCF7 Function assay 48 hrs Inhibition of chemoattractant-induced cell migration of human MCF7 cells after 48 hrs by transwell migration assay, IC50=0.0004μM 16520733
COS7 Function assay Displacement of E2-Alexa633 from GFP-tagged GPR30 expressed in COS7 cells by FACS, Ki=0.0057μM 16520733
COS7 Function assay 1 nM Agonist activity at GFP-tagged ERalpha expressed in COS7 cells assessed as increase in intracellular calcium level at 1 nM by spectrofluorimetry 16520733
COS7 Function assay 1 nM Agonist activity at GFP-tagged ERbeta expressed in COS7 cells assessed as increase in intracellular calcium level at 1 nM by spectrofluorimetry 16520733
COS7 Function assay 1 nM Agonist activity at GFP-tagged ERalpha expressed in COS7 cells assessed as PI3K activation at 1 nM by PIP3 nuclear accumulation assay 16520733
COS7 Function assay 1 uM Agonist activity at GFP-tagged ERbeta expressed in COS7 cells assessed as PI3K activation at 1 nM by PIP3 nuclear accumulation assay 16520733
COS7 Function assay 1 uM Agonist activity at GFP-tagged GPR30 expressed in COS7 cells assessed as PI3K activation at 1 nM by PIP3 nuclear accumulation assay 16520733
COS7 Function assay 1 nM Binding affinity to mRFP1-tagged GPR30 expressed in COS7 cells coexpressing GFP-tagged ERalpha assessed as inhibition of E2-Alexa633 binding in nucleus at 1 uM by FACS 16520733
COS7 Function assay 1 nM Binding affinity to GFP-tagged ERalpha expressed in COS7 cells coexpressing mRFP1-tagged GPR30 assessed as inhibition of E2-Alexa633 binding in nucleus at 1 uM by FACS 16520733
MCF7 Function assay 1 nM 24 hrs Down regulation of estrogen receptor expression in MCF7 cells at 1 nM after 24 hrs 17275315
HEK293 Function assay Agonist activity at human recombinant ERalpha expressed in HEK293 cells by transactivation assay, EC50=0.00075μM 17448656
HEK293 Function assay Agonist activity at human recombinant ERbeta expressed in HEK293 cells by transactivation assay, EC50=0.0021μM 17448656
HEK293 Function assay Agonist activity at ERalpha expressed in HEK293 cells by transactivation assay, EC50=0.00075μM 17890084
HEK293 Function assay Agonist activity at ERbeta expressed in HEK293 cells by transactivation assay, EC50=0.0021μM 17890084
MCF7 BUS Function assay Estrogenic potency in human MCF7 BUS cells assessed as drug level inducing maximal cell proliferation, MED=0.001μM 18242997
CHO Function assay Agonist activity at human TGR5 expressed in CHO cells by luciferase assay, EC50=38.4μM 18307294
MCF7 Function assay 6 days Estrogenic activity in human MCF7 cells assessed as cell proliferation after 6 days by WST8 assay, EC50=0.0000037μM 18760603
HEC1 Function assay 24 hrs Agonist activity at full-length human estrogen receptor beta expressed in human HEC1 cells assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay, EC50=0.00013μM 19128016
HEC1 Function assay 24 hrs Agonist activity at full-length human estrogen receptor alpha expressed in human HEC1 cells assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay, EC50=0.0007μM 19128016
HEC1 Function assay 24 hrs Agonist activity at ERalpha expressed in human HEC1 cells assessed as transcriptional potency after 24 hrs by luciferase-beta galactosidase reporter gene assay, EC50=0.0001μM 19286283
HEC1 Function assay 24 hrs Agonist activity at ERbeta expressed in human HEC1 cells assessed as transcriptional potency after 24 hrs by luciferase-beta galactosidase reporter gene assay, EC50=0.0005μM 19286283
BL21(DE3) Function assay Agonist activity at human ERalpha ligand binding domain expressed in Escherichia coli BL21(DE3) cells assessed as induction of coactivator 53-protein binding by fluorescence assay 19561619
BL21(DE3) Function assay Agonist activity at human ERbeta ligand binding domain expressed in Escherichia coli BL21(DE3) cells assessed as induction of coactivator 53-protein binding by fluorescence assay 19561619
SF9 Function assay Displacement of [3H]17beta-estradiol from human ERalpha expressed in SF9 cells, IC50=0.0125μM 19836949
COS7 Function assay Agonist activity at estrogen receptor alpha ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay, EC50=0.0032μM 19863083
COS7 Function assay Agonist activity at estrogen receptor beta ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay, EC50=0.011μM 19863083
MCF7:WS8 Function assay 7 days Estrogenic activity in human ERalpha expressing MCF7:WS8 cells assessed as stimulation of cell proliferation after 7 days, EC50=0.000001μM 20334368
MCF7:WS8 Function assay Activation of human ER in human MCF7:WS8 cells expressing estrogen responsive element by luciferase reporter gene assay 20334368
T47D:C:4:2 Function assay Estrogenic activity at wild type ER alpha expressed in T47D:C:4:2 cells coexpressing estrogen response element by duel luciferase reporter gene assay 20334368
T47D:C:4:2 Function assay Estrogenic activity at wild type ER alpha D351G mutant expressed in T47D:C:4:2 cells coexpressing estrogen response element by duel luciferase reporter gene assay 20334368
HEK293 Function assay 18 hrs Transactivation of human ERbeta expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay, EC50=0.0000617μM 20408532
HEK293 Function assay 18 hrs Transactivation of human ERalpha expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay, EC50=0.0000646μM 20408532
CHO-K1 Function assay Agonist activity at ERbeta expressed in CHO-K1 cells by luciferase reporter gene transactivation assay, EC50=0.03μM 20553023
CHO-K1 Function assay Agonist activity at ERalpha expressed in CHO-K1 cells by luciferase reporter gene transactivation assay, EC50=0.05μM 20553023
HeLa Function assay 18 hrs Displacement of [2,4,6,7-3H]estradiol from human ERalpha expressed in HeLa cells after 18 hrs by liquid scintillation counting, Ki=0.00016μM 20621492
HEK293T Function assay Agonist activity at human ERalpha E353A mutant expressed in HEK293T cells co-expressing ERE assessed as transactivation activity by luciferase reporter gene assay, EC50=0.0025μM 20659801
HEK293T Function assay Agonist activity at human ERbeta E305A mutant expressed in HEK293T cells co-expressing ERE assessed as transactivation activity by luciferase reporter gene assay, EC50=0.0104μM 20659801
HeLa Function assay Agonist activity at human wild type ERalpha expressed in human HeLa cells co-expressing ERE assessed as transactivation activity by luciferase reporter gene assay 20659801
HeLa Function assay Transactivation of human wild type ERalpha expressed in human HeLa cells co-expressing AP-1 by luciferase reporter gene assay 20659801
HeLa Function assay Agonist activity at human wild type ERbeta expressed in human HeLa cells co-expressing ERE assessed as transactivation activity by luciferase reporter gene assay 20659801
HeLa Function assay Antagonist activity at human wild type ERbeta expressed in human HeLa cells co-expressing AP-1 assessed as inhibition of transactivation activity by luciferase reporter gene assay 20659801
U2OS Function assay 18 hrs Agonist activity at ERbeta-LBD in human U2OS cells transfected with Gal4-DBD assessed as increase of transactivation activity after 18 hrs by luciferase reporter gene assay, EC50=0.0004581μM 20812681
U2OS Function assay 18 hrs Agonist activity at ERalpha-LBD in human U2OS cells transfected with Gal4-DBD assessed as increase of transactivation activity after 18 hrs by luciferase reporter gene assay, EC50=0.002773μM 20812681
U2OS Function assay 18 hrs Antagonist activity at ERbeta-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity after 18 hrs by luciferase reporter gene assay, IC50=0.01074μM 20812681
U2OS Function assay 18 hrs Antagonist activity at ERalpha-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity after 18 hrs by luciferase reporter gene assay, IC50=0.02104μM 20812681
HEK293 Function assay Agonist activity at ZFP-fused ERRbeta LBD expressed in HEK293 cells by TR-FRET assay, EC50=0.0046μM 21218783
MCF7 Function assay up to 6 days Agonist activity at human ERalpha LBD in human MCF7 cells assessed as induction of cell proliferation after up to 6 days by celltiter-glo assay, EC50=0.01μM 21218783
MCF7 Cytotoxicity assay 4 uM 24 hrs Cytotoxicity against human MCF7 cells at 4 uM after 24 hrs by MTT assay 21459581
MCF7 Function assay 4 uM 24 hrs Reduction in Cdk1 protein level in human MCF7 cells at 4 uM after 24 hrs by Western blot analysis 21459581
HEC1 Function assay 24 hrs Agonist activity at human full-length ERalpha receptor expressed in human HEC1 cells co-expressing (ERE)2-pS2-luc gene assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay, EC50=0.00009μM 21481497
HEC1 Function assay 24 hrs Agonist activity at human full-length ERbeta receptor expressed in human HEC1 cells co-expressing (ERE)2-pS2-luc gene assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay, EC50=0.00072μM 21481497
MCF7 Function assay 0.01 nM 48 hrs Estrogenic activity in human ER-positive MCF7 cells assessed as secreted alkaline phosphatase activity at 0.01 nM after 48 hrs by phospha-light reporter chemiluminescence assay 21800859
HEK Function assay 18 hrs Agonist activity at ERalpha expressed in HEK cells co-expressing beta-lactamase after 18 hrs by beta-lactamase reporter gene assay, EC50=0.000046μM 21885279
UAS Function assay 18 hrs Agonist activity at ERbeta expressed in UAS cells co-expressing beta-lactamase after 18 hrs by beta-lactamase reporter gene assay, EC50=0.00025μM 21885279
HEC-1 Function assay 24 hrs Agonist activity at human ERalpha expressed in HEC-1 cells coexpressing beta-gal assessed as luciferase activity after 24 hrs by reporter gene assay, EC50=0.000123μM 22122563
U2OS Function assay 24 hrs Agonist activity at human ERalpha expressed in U2OS cells coexpressing pCMX-hSRC3 assessed as luciferase activity after 24 hrs by reporter gene assay, EC50=0.00015μM 22122563
HEC-1 Function assay 24 hrs Agonist activity at human ERbeta expressed in HEC-1 cells coexpressing beta-gal assessed as luciferase activity after 24 hrs by reporter gene assay, EC50=0.0002μM 22122563
U2OS Function assay 24 hrs Agonist activity at human ERbeta expressed in U2OS cells coexpressing pCMX-hSRC3 assessed as luciferase activity after 24 hrs by reporter gene assay, EC50=0.0004μM 22122563
BL21 Function assay 1 hr Agonist activity at human N-His6-tagged terbium-labelled NRID-SRC3 of ERalpha ligand binding domain expressed in Escherichia coli BL21 cells after 1 hr by TR-FRET assay, EC50=0.00056μM 22122563
BL21 Function assay 1 hr Agonist activity at human N-His6-tagged terbium-labelled NRID-SRC3 of ERbeta ligand binding domain expressed in Escherichia coli BL21 cells after 1 hr by TR-FRET assay, EC50=0.0009μM 22122563
BL21 Function assay 1 hr Agonist activity at human N-His6-tagged terbium-labelled ERbeta ligand binding domain expressed in Escherichia coli BL21 cells assessed as recruitment of fluorescein-labelled SRC3 after 1 hr by TR-FRET assay, EC50=0.0015μM 22122563
BL21 Function assay 1 hr Agonist activity at human N-His6-tagged terbium-labelled ERalpha ligand binding domain expressed in Escherichia coli BL21 cells assessed as recruitment of fluorescein-labelled SRC3 after 1 hr by TR-FRET assay, EC50=0.003μM 22122563
Ishikawa cells Function assay 3 days Agonist activity at estrogen receptor in human Ishikawa cells assessed as increase of alkaline phosphatase level after 3 days using P-nitrophenyl phosphate as substrate, EC50=0.0009μM 22178552
HepG2 Function assay 24 hrs Agonist activity at human ERalpha expressed in HepG2 cells after 24 hrs by luciferase reporter gene assay, EC50=0.0022μM 22283328
HepG2 Function assay 24 hrs Agonist activity at human ERbeta expressed in HepG2 cells after 24 hrs by luciferase reporter gene assay, EC50=0.011μM 22283328
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against estrogen-deficient human MCF7 cells after 72 hrs by MTT assay, EC50=0.0000064μM 22464681
MCF7:D5L Function assay 16 hrs Estrogenic activity at estrogen receptor in human MCF7:D5L cells co-expressing ERE assessed as induction of luciferase gene expression after 16 hrs by microplate reader, EC50=0.0000196μM 22464681
Ishikawa cells Function assay 72 hrs Estrogenic activity at estrogen receptor in human Ishikawa cells assessed as induction of alkaline phosphatase expression after 72 hrs by microplate reader, EC50=0.0000246μM 22464681
Ishikawa cells Function assay 0.1 nM 72 hrs Effect on cell proliferation of human Ishikawa cells at 0.1 nM after 72 hrs by MTT assay 22464681
CHO-K1 Function assay 24 hrs Transcriptional activation of ERbeta receptor expressed in CHO-K1 cells after 24 hrs by luciferase reporter gene assay, EC50=0.000036μM 22647217
CHO-K1 Function assay 24 hrs Transcriptional activation of ERalpha receptor expressed in CHO-K1 cells after 24 hrs by luciferase reporter gene assay, EC50=0.00005μM 22647217
yeast AH109 Function assay 24 hrs Agonist activity at ERalpha receptor LBD expressed in yeast AH109 cells assessed as compound concentration at which 10% agonist activity of the maximum activity of E2 after 24 hrs by alpha-galactosidase assay, Activity=0.0001μM 22647217
yeast AH109 Function assay 24 hrs Agonist activity at ERbeta receptor LBD expressed in yeast AH109 cells assessed as compound concentration at which 10% agonist activity of the maximum activity of E2 after 24 hrs by alpha-galactosidase assay, Activity=0.00018μM 22647217
yeast AH109 Function assay 24 hrs Agonist activity at ERalpha receptor LBD expressed in yeast AH109 cells assessed as interaction with SRC1 after 24 hrs by alpha-galactosidase assay, EC50=0.00105μM 22647217
yeast AH109 Function assay 24 hrs Agonist activity at ERbeta receptor LBD expressed in yeast AH109 cells assessed as interaction with SRC1 after 24 hrs by alpha-galactosidase assay, EC50=0.00108μM 22647217
U2-OS Function assay Activation of human ERalpha expressed in human U2-OS cells by luciferase reporter gene assay relative to untreated control, EC50=0.000004μM 23043242
U2-OS Function assay Activation of human ERbeta expressed in human U2-OS cells by luciferase reporter gene assay relative to untreated control, EC50=0.00001μM 23043242
MCF7/2a Function assay Activation of ERalpha in human MCF7/2a cells by luciferase reporter gene assay relative to untreated control, EC50=0.0001μM 23043242
MCF7 Function assay 1 uM Down regulation of ERalpha human MCF7 cells at 1 uM by Western blotting 23043242
HeLa Function assay 1 nM 20 to 24 hrs Agonist activity at ERalpha receptor in human HeLa cells assessed as activation of ERalpha-based transcription at 1 nM after 20 to 24 hrs by luciferase reporter gene assay 23448346
MCF7 Function assay 1 nM 20 to 24 hrs Agonist activity at ERalpha receptor in human MCF7 cells assessed as activation of ERalpha-based transcription at 1 nM after 20 to 24 hrs by luciferase reporter gene assay 23448346
MCF7:WS8 Function assay 48 hrs Agonist activity at ER in human MCF7:WS8 cells assessed as increase in pS2 gene expression at 10'-10 M after 48 hrs by RT-PCR analysis 24805199
MCF7:WS8 Function assay 48 hrs Agonist activity at ER in human MCF7:WS8 cells assessed as increase in GREB1 gene expression at 10'-10 M after 48 hrs by RT-PCR analysis 24805199
MCF7:WS8 Function assay 48 hrs Agonist activity at ER in human MCF7:WS8 cells assessed as increase in PgR gene expression at 10'-10 M after 48 hrs by RT-PCR analysis 24805199
MCF7 Antiproliferative assay 2 days Antiproliferative activity human ER-positive MCF7 cells after 2 days by MTT assay, IC50=27.35μM 25222876
MDA-MB-231 Antiproliferative assay 2 days Antiproliferative activity human ER-negative MDA-MB-231 cells after 2 days by MTT assay, IC50=33.46μM 25222876
B16F10 Antiproliferative assay 2 days Antiproliferative activity mouse B16F10 cells after 2 days by MTT assay, IC50=39.81μM 25222876
MIAPaCa2 Antiproliferative assay 2 days Antiproliferative activity human MIAPaCa2 cells after 2 days by MTT assay, IC50=42.93μM 25222876
HEK293 Function assay Agonist activity at human ERalpha expressed in HEK293 cells by luciferase reporter gene assay, EC50=0.000024μM 25305688
HEK293 Function assay Agonist activity at human ERbeta expressed in HEK293 cells by luciferase reporter gene assay, EC50=0.000085μM 25305688
MCF7 Function assay 24 hrs Agonist activity at human ERalpha in human MCF7 cells assessed as progesterone receptor endogenous genes activation after 24 hrs by qPCR, EC50=0.0000084μM 25559213
HEC1 Function assay 24 hrs Agonist activity at human ERalpha expressed in human HEC1 cells assessed as transcriptional activation after 24 hrs by ERE-luciferase reporter gene transfection assay, EC50=0.00016μM 25559213
MCF7 Function assay 24 hrs Agonist activity at human ERbeta in human MCF7 cells assessed as otubain 2 endogenous genes activation after 24 hrs by qPCR, EC50=0.0003μM 25559213
HEC1 Function assay 24 hrs Agonist activity at human ERbeta expressed in human HEC1 cells assessed as transcriptional activation after 24 hrs by ERE-luciferase reporter gene transfection assay, EC50=0.00038μM 25559213
MCF7 Function assay 10 nM 20 hrs Induction of estrogen receptor-alpha degradation in human MCF7 cells at 10 nM after 20 hrs by Western blot analysis 25879485
Saos2 Function assay 1 uM 7 days Agonist activity at ERalpha in human Saos2 cells assessed as induction of cell proliferation at 1 uM after 7 days by MTS assay 27155470
Saos2 Function assay 0.1 nM 3 days Agonist activity at ERalpha in human Saos2 cells assessed as increase in ALP activity using p-nitrophenyl phosphate as substrate at 0.1 nM after 3 days by colorimetric assay 27155470
insect cells Function assay Displacement of Fluormone ES2 Green from human recombinant full length ERalpha expressed in insect cells measured up to 4 hrs by fluorescence polarization assay, IC50=0.0044μM 27647375
insect cells Function assay 2 hrs Displacement of fluormone-labeled ES2 from recombinant full length human ERalpha ligand binding domain expressed in insect cells after 2 hrs by TR-FRET assay, IC50=0.00041μM 28105283
insect cells Function assay Inhibition of fluormone ES2 binding to recombinant full length human ERbeta expressed in insect cells by fluorescence polarization assay, IC50=0.00665μM 28735214
Ishikawa cells Function assay 96 hrs Estrogenic activity at estrogen receptor alpha in human Ishikawa cells assessed as induction of alkaline phosphatase activity using p-Nitrophenol phosphate as substrate pretreated for 96 hrs followed by substrate addition measured every 15 secs by scannin, EC50=0.0002μM 28812892
293 cells Function assay Binding affinity to ER (unknown origin) expressed in UAS-bla GripTite 293 cells by Select screen competitive binding assay, EC50=0.0023μM 28886996
HEk293 Function assay Agonist activity at recombinant human GAL4-fused ERalpha expressed in HEk293 cells by luciferase reporter gene assay, EC50=0.00011μM 29525335
Ishikawa Function assay 96 hrs Estrogenic activity at ERalpha in human Ishikawa cells assessed as induction of alkaline phosphatase activity using p-nitrophenol as substrate treated for 96 hrs followed by substrate addition by spectrophotometric method, EC50=0.00003μM 29641206
MDA-MB-231/beta41 Function assay 18 hrs Estrogenic activity at ERbeta (unknown origin) expressed in human MDA-MB-231/beta41 cells after 18 hrs by renilla luciferase reporter gene assay, EC50=0.00003μM 29641206
insect cells Function assay 2 hrs Inhibition of fluoromone binding to recombinant human full length untagged ERbeta expressed in insect cells after 2 hrs by fluorescence polarization assay, IC50=0.00128μM 29869503
insect cells Function assay 2 hrs Inhibition of fluoromone binding to recombinant human full length untagged ERalpha expressed in insect cells after 2 hrs by fluorescence polarization assay, IC50=0.004804μM 29869503
insect cells Function assay 0.1 to 10000 uM Binding affinity to untagged human recombinant full length ERalpha expressed in insect cells 0.1 to 10000 uM by Fluormone ES2 Green displacement based assay 30091920
293 cells Function assay Agonist activity at GAL4 DNA-binding domain fused ERalpha (unknown origin) ligand binding domain expressed in UAS-bla GripTite 293 cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay, IC50=0.000107μM 30144697
293 cells Function assay Agonist activity at GAL4 DNA-binding domain fused ERbeta (unknown origin) ligand binding domain expressed in UAS-bla GripTite 293 cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay, IC50=0.000579μM 30144697
HEK293 Function assay Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalpha degradation by luciferase reporter gene assay, EC50=0.00009μM 30940565
HEK293 Function assay Agonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ER-alpha-mediated transcriptional activity by luciferase reporter gene assay, EC50=0.00013μM 30940565
Sf9 Function assay Binding Assay: The method employed was adapted from the scientific literature and described in detail by Osbourn et al. (1993, Biochemistry, 32, 6229-6236). Recombinant human ERalpha and ERR proteins were purified from transfected Sf9-cells. The in vitro , Ki=0.000015μM ChEMBL
Sf9 Function assay Inhibition Assay: The method employed was adapted from the scientific literature and described in detail by Osboum et al. (1993, Biochemistry, 32, 6229-6236). Recombinant human ERalpha and ERbeta proteins were purified from transfected Sf9-cells. The in v, Ki=0.000015μM ChEMBL
HEK293T Function assay 24 hrs Agonist activity at ER-beta (unknown origin) transfected in HEK293T cells after 24 hrs by Steady-Glo luciferase reporter gene assay, EC50=0.0000398μM ChEMBL
HEK293T Function assay 24 hrs Agonist activity at ER-alpha (unknown origin) transfected in HEK293T cells after 24 hrs by Steady-Glo luciferase reporter gene assay, EC50=0.0001μM ChEMBL
Sf9 Function assay Binding Assay: The method employed was adapted from the scientific literature and described in detail by Osbourn et al. (1993, Biochemistry, 32, 6229-6236). Recombinant human ERalpha and ERR proteins were purified from transfected Sf9-cells. The in vitro , Ki=0.00021μM ChEMBL
Sf9 Function assay Inhibition Assay: The method employed was adapted from the scientific literature and described in detail by Osboum et al. (1993, Biochemistry, 32, 6229-6236). Recombinant human ERalpha and ERbeta proteins were purified from transfected Sf9-cells. The in v, Ki=0.00021μM ChEMBL
CV-1 Luciferase Assay Luciferase Assay: Estrogen receptor-negative CV-1 kidney cells are maintained in Dulbecco's modified Eagle's medium with 4.5 g/L glucose supplemented with 10% fetal bovine serum and 100 units/ml penicillin-streptomycin at 37° C. in a humidified 5% CO2 atm, IC50=0.0017μM ChEMBL
CV-1 Luciferase Assay Luciferase Assay: Estrogen receptor-negative CV-1 kidney cells are maintained in Dulbecco's modified Eagle's medium with 4.5 g/L glucose supplemented with 10% fetal bovine serum and 100 units/ml penicillin-streptomycin at 37° C. in a humidified 5% CO2 atm, IC50=0.0019μM ChEMBL
COS7 Function assay Competitive binding affinity to G-protein coupled estrogen receptor (unknown origin) expressed in COS7 cells by E2 Alexa 633 staining based fluorescence analysis, Ki=0.0027μM ChEMBL
MDA-MB-231 Growth inhibition assay 1 pM to 1 μM 48 hr Growth inhibition of Homo sapiens (human) MDA-MB-231 cells at 10'-12 to 10'-6 M after 48 hr by MTT assay ChEMBL
UMR106 Function assay 10 nM 24 hrs Transactivation of human ER-alpha transfected in rat UMR106 cells at 10'-8 M after 24 hrs by dual luciferase reporter gene assay ChEMBL
UMR106 Function assay 10 nM 24 hrs Transactivation of human ER-beta transfected in rat UMR106 cells at 10'-8 M after 24 hrs by dual luciferase reporter gene assay ChEMBL
U2OS Function assay 0.01 uM 24 hrs Activation of ERbeta (unknown origin) expressed in human U2OS cells at 0.01 uM incubated for 24 hrs by luciferase reporter gene assay ChEMBL
U2OS Function assay 0.01 uM 24 hrs Activation of ERalpha (unknown origin) expressed in human U2OS cells at 0.01 uM incubated for 24 hrs by luciferase reporter gene assay ChEMBL
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Solubility

In vitro
Batch:

DMSO : 54 mg/mL (198.25 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 54 mg/mL

Water : Insoluble

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% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 272.38 Formula

C18H24O2

 Storage (From the date of receipt)
CAS No. 50-28-2 Download SDF Storage of Stock Solutions

Synonyms 17β-estradiol, β-Estradiol, E2, 17β-Oestradiol Smiles CC12CCC3C(C1CCC2O)CCC4=C3C=CC(=C4)O

Mechanism of Action

Targets/IC50/Ki
Estrogen receptor
In vitro

Estradiol induces new dendritic spines and synapses on hippocampal CA1 pyramidal cells. This compound treatment resulted in a 46% increase in NMDA receptor binding. It increases NMDA receptor binding in parallel with dendritic spine and synapse density. This chemical treatment results in increased sensitivity of CA1 pyramidal cells to NMDA receptor-mediated synaptic input and that this increase is well correlated with the estradiol-induced increase in dendritic spine density in the apical dendritic tree of these cells.

This compound is found to reduce Ba2+ entry reversibly via Ca2+ channels in acutely dissociated and cultured neostriatal neurons. 17 alpha-Estradiol also reduces Ba2+ currents but is significantly less effective than 17 beta-estradiol in rat neostriatal neurons.

It exerts a dose-dependent inhibition of IL-1-, TNF-, and IL-1 and TNF-induced production of bioassayable IL-6. This chemical inhibits both TNF-induced IL-6 production and osteoclast development in primary bone cell cultures derived from neonatal murine calvaria.

In vivo

Estradiol mediates fluctuation in hippocampal synapse density during the estrous cycle in the adult rat.

This compound alone can reverse the ovariectomy-induced decrease in spine density. It combined with Progesterone initially increases spine density for a period of 2 to 6 hours but then results in a much sharper decrease than is observed following this chemical alone.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/1613547/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8245220/

Applications

Methods Biomarkers Images PMID
Western blot p-GSK3β / GSK3 β-catenin Survivin / ER-alpha / NgBR ERα / FOXP1 / KRAS / PTEN
S1709-WB1
19360103

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05900895 Not yet recruiting
Metastatic Breast Cancer
Mary D Chamberlin|Dartmouth-Hitchcock Medical Center
 May 2024 Phase 1
NCT06380205 Recruiting
Healthy Participants
Incyte Corporation
 May 7 2024 Phase 1
NCT06334315 Not yet recruiting
Contraception|Pharmacogenomic Drug Interaction
Yale University|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)
 May 2024 Phase 4

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