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17β-Estradiol Metabolita Endogeno Umano

Name: 17β-Estradiol
Brand: Selleck Chemicals
SKU: S1709
Rating: 5 (27 reviews)

N. Cat.S1709

Estradiol (17β-estradiolo, β-Estradiolo, E2, 17β-Oestradiolo) è un ormone sessuale umano e uno steroide, nonché il principale ormone sessuale femminile. Estradiol regola positivamente l'espressione di IL-6 attraverso la via del recettore degli estrogeni β (ERβ).

17β-Estradiol Endogenous Metabolite inibitore Chemical Structure

Struttura chimica

Peso molecolare: 272.38

Vai a

Controllo Qualità

Lotto: Purezza: 99.99%

99.99

Target correlati	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Altro Endogenous Metabolite Inibitori	4-HNE (4-Hydroxynonenal) Heparan Sulfate Ademetionine (S-Adenosylmethionine) Sodium L-lactate 3-Hydroxybutyric acid (BHB acid)

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dellattività	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
Clicca per visualizzare più dati sperimentali sulle linee cellulari

Informazioni chimiche, conservazione e stabilità

Peso molecolare	272.38	Formula	C₁₈H₂₄O₂	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	50-28-2	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	17β-estradiol, β-Estradiol, E2, 17β-Oestradiol			Smiles	CC12CCC3C(C1CCC2O)CCC4=C3C=CC(=C4)O

Solubilità

In vitro
Lotto:

DMSO : 54 mg/mL (198.25 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 54 mg/mL

Water : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	2.700mg/ml (9.91mM)	Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 54 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Targets/IC₅₀/Ki	Estrogen receptor
In vitro	Estradiol induce nuove spine dendritiche e sinapsi sulle cellule piramidali CA1 dell'ippocampo. Questo trattamento con il composto ha portato a un aumento del 46% nel legame del recettore NMDA. Aumenta il legame del recettore NMDA in parallelo con la densità delle spine dendritiche e delle sinapsi. Questo trattamento chimico si traduce in una maggiore sensibilità delle cellule piramidali CA1 all'input sinaptico mediato dal recettore NMDA e che questo aumento è ben correlato con l'aumento indotto dall'estradiolo della densità delle spine dendritiche nell'albero dendritico apicale di queste cellule. Questo composto è stato trovato per ridurre reversibilmente l'ingresso di Ba2+ tramite i canali Ca2+ nei neuroni neostriatali acutamente dissociati e coltivati. Il 17 alfa-Estradiol riduce anche le correnti di Ba2+ ma è significativamente meno efficace del 17 beta-estradiolo nei neuroni neostriatali di ratto. Esercita un'inibizione dose-dipendente della produzione di IL-6 bioassayabile indotta da IL-1, TNF e IL-1 e TNF. Questa sostanza chimica inibisce sia la produzione di IL-6 indotta dal TNF che lo sviluppo degli osteoclasti in colture primarie di cellule ossee derivate da calotte craniche murine neonatali.
In vivo	Estradiol media la fluttuazione della densità delle sinapsi ippocampali durante il ciclo estrale nel ratto adulto. Questo composto da solo può invertire la diminuzione della densità delle spine indotta dall'ovariectomia. Combinato con il Progesterone, inizialmente aumenta la densità delle spine per un periodo da 2 a 6 ore ma poi porta a una diminuzione molto più marcata di quella osservata dopo questa sostanza chimica da sola.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/9030643/ [2] https://pubmed.ncbi.nlm.nih.gov/8551343/ [3] https://pubmed.ncbi.nlm.nih.gov/1541679/ [4] https://pubmed.ncbi.nlm.nih.gov/1613547/ [5] https://pubmed.ncbi.nlm.nih.gov/8245220/

Applicazioni

Metodi	Biomarcatori	Immagini	PMID
Western blot	p-GSK3β / GSK3 β-catenin Survivin / ER-alpha / NgBR ERα / FOXP1 / KRAS / PTEN		19360103

Informazioni sullo studio clinico

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
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

Supporto tecnico

Istruzioni per la manipolazione

Tel: +1-832-582-8158 Ext:3

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