U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C18H24O2
Molecular Weight 272.3826
Optical Activity ( + )
Defined Stereocenters 5 / 5
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ESTRADIOL

SMILES

C[C@@]12CC[C@]3([H])c4ccc(cc4CC[C@@]3([H])[C@]2([H])CC[C@]1([H])O)O

InChI

InChIKey=VOXZDWNPVJITMN-ZBRFXRBCSA-N
InChI=1S/C18H24O2/c1-18-9-8-14-13-5-3-12(19)10-11(13)2-4-15(14)16(18)6-7-17(18)20/h3,5,10,14-17,19-20H,2,4,6-9H2,1H3/t14-,15-,16+,17+,18+/m1/s1

HIDE SMILES / InChI

Molecular Formula C18H24O2
Molecular Weight 272.3826
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 5 / 5
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/020375s027lbl.pdf

Estradiol an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids. In humans, it is produced primarily by the cyclic ovaries and the placenta. It is also produced by the adipose tissue of men and postmenopausal women. The 17-alpha-isomer of estradiol binds weakly to estrogen receptors (receptors, estrogen) and exhibits little estrogenic activity in estrogen-responsive tissues. Estradiol enters target cells freely (e.g., female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estradiol is used for the treatment of urogenital symptoms associated with post-menopausal atrophy of the vagina (such as dryness, burning, pruritus and dyspareunia) and/or the lower urinary tract (urinary urgency and dysuria). Estradiol is marketed under the brand name Climara (among others), indicated for: the treatment of moderate to severe vasomotor symptoms due to menopause, treatment of symptoms of vulvar and vaginal atrophy due to menopause, treatment of hypoestrogenism due to hypogonadism, castration or primary ovarian failure and prevention of postmenopausal osteoporosis.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P08842
Gene ID: 412
Gene Symbol: STS
Target Organism: Homo sapiens (Human)
0.00839999999999999948 nM [EC50]
1.39999999999999991 nM [EC50]
19.1000000000000014 nM [IC50]
0.130000000000000004 nM [Ki]
0.0899999999999999967 nM [Kd]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
CLIMARA

Approved Use

Climara is an estrogen indicated for: •Treatment of Moderate to Severe Vasomotor Symptoms due to Menopause •Treatment of Moderate to Severe Symptoms of Vulvar and Vaginal Atrophy due to Menopause •Treatment of Hypoestrogenism due to Hypogonadism, Castration or Primary Ovarian Failure •Prevention of Postmenopausal Osteoporosis

Launch Date

157680000000
Preventing
CLIMARA

Approved Use

Climara is an estrogen indicated for: •Treatment of Moderate to Severe Vasomotor Symptoms due to Menopause •Treatment of Moderate to Severe Symptoms of Vulvar and Vaginal Atrophy due to Menopause •Treatment of Hypoestrogenism due to Hypogonadism, Castration or Primary Ovarian Failure •Prevention of Postmenopausal Osteoporosis

Launch Date

157680000000
Primary
CLIMARA

Approved Use

Climara is an estrogen indicated for: •Treatment of Moderate to Severe Vasomotor Symptoms due to Menopause •Treatment of Moderate to Severe Symptoms of Vulvar and Vaginal Atrophy due to Menopause •Treatment of Hypoestrogenism due to Hypogonadism, Castration or Primary Ovarian Failure •Prevention of Postmenopausal Osteoporosis

Launch Date

157680000000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
14.7 pg/mL
0.25 mg 1 times / day steady-state, topical
dose: 0.25 mg
route of administration: Topical
experiment type: STEADY-STATE
co-administered:
ESTRADIOL plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE
food status: UNKNOWN
92 pg/mL
0.05 mg 1 times / day multiple, topical
dose: 0.05 mg
route of administration: Topical
experiment type: MULTIPLE
co-administered:
ESTRADIOL plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
236 pg × h/mL
0.25 mg 1 times / day steady-state, topical
dose: 0.25 mg
route of administration: Topical
experiment type: STEADY-STATE
co-administered:
ESTRADIOL plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
10 h
0.25 mg 1 times / day steady-state, topical
dose: 0.25 mg
route of administration: Topical
experiment type: STEADY-STATE
co-administered:
ESTRADIOL plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE
food status: UNKNOWN
1.75 h
0.05 mg 1 times / day multiple, topical
dose: 0.05 mg
route of administration: Topical
experiment type: MULTIPLE
co-administered:
ESTRADIOL plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE
food status: UNKNOWN
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG



Drug as perpetrator​

Drug as perpetrator​

Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
minor
minor
minor
minor
minor
minor
no
no
no
no
no
no
no
no
no
yes [Km 7 uM]
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Effect of estradiol benzoate on the proliferation of osteogenic cells in fetal rat fibulae cultured in vitro.
1978 Mar
An increase of pituitary 3', 5' cyclic adenosine monophosphate produced by estradiol benzoate in vitro: possible implication of this increase in the secretion of luteinizing hormone.
1978 May
Sulfation of estrone and 17 beta-estradiol in human liver. Catalysis by thermostable phenol sulfotransferase and by dehydroepiandrosterone sulfotransferase.
1992 May-Jun
[The effect of adrenaline and 17beta-estradiol sulfate on transmembrane potentials of guinea pig cardiomyocytes].
1996 Dec
Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
1997 Mar
Indole-3-carbinol is a negative regulator of estrogen receptor-alpha signaling in human tumor cells.
2000 Dec
Estrogen activation of the nuclear orphan receptor CAR (constitutive active receptor) in induction of the mouse Cyp2b10 gene.
2000 Nov
Estradiol enhances the resistance of LDL to oxidation by stabilizing apoB-100 conformation.
2000 Nov 14
Relative binding affinity does not predict biological response to xenoestrogens in rat endometrial adenocarcinoma cells.
2000 Oct
Resveratrol acts as a mixed agonist/antagonist for estrogen receptors alpha and beta.
2000 Oct
Constitutive expression of the steroid sulfatase gene supports the growth of MCF-7 human breast cancer cells in vitro and in vivo.
2001 Apr
Hormone status selects for spontaneous somatic androgen receptor variants that demonstrate specific ligand and cofactor dependent activities in autochthonous prostate cancer.
2001 Apr 6
Vitellogenin-induced pathology in male summer flounder (Paralichthys dentatus).
2001 Feb
Use of salivary biomarkers in biobehavioral research: cotton-based sample collection methods can interfere with salivary immunoassay results.
2001 Feb
Estrogen induces the Akt-dependent activation of endothelial nitric-oxide synthase in vascular endothelial cells.
2001 Feb 2
Effects of follicle-stimulating hormone with and without luteinizing hormone on serum hormone concentrations, follicle growth, and intrafollicular estradiol and aromatase activity in gonadotropin-releasing hormone-immunized heifers.
2001 Jan
Female steroid hormones modulate receptors for nerve growth factor in rat dorsal root ganglia.
2001 Jan
Regulation and role of vascular endothelial growth factor in the corpus luteum during mid-pregnancy in rats.
2001 Jan
Increased expression of a novel heat shock protein transcript in the mouse uterus during decidualization and in response to progesterone.
2001 Jan
Regulation of progesterone receptors and decidualization in uterine stroma of the estrogen receptor-alpha knockout mouse.
2001 Jan
Pregnancy stimulates secretion of adrenocorticotropin and nitric oxide from peripheral bovine lymphocytes.
2001 Jan
Estradiol-induced attenuation of pulmonary hypertension is not associated with altered eNOS expression.
2001 Jan
Comparison of histological compositions and apoptosis in canine spontaneous benign prostatic hyperplasia treated with androgen suppressive agents chlormadinone acetate and finasteride.
2001 Jan
Metabolism of estradiol, ethynylestradiol, and moxestrol in rat uterus, vagina, and aorta: influence of sex steroid treatment.
2001 Jan
Rapid and reversible inhibition of brain aromatase activity.
2001 Jan
Oestrogen-induced changes in the synaptology of the monkey (Cercopithecus aethiops) arcuate nucleus during gonadotropin feedback.
2001 Jan
Stimulatory effect of clofibrate and gemfibrozil administration on the formation of fatty acid esters of estradiol by rat liver microsomes.
2001 Jan
Influence of gender and sex hormones on nicotine acute pharmacological effects in mice.
2001 Jan
Heat-shock factor-1, steroid hormones, and regulation of heat-shock protein expression in the heart.
2001 Jan
Gender-related distinctions in protein kinase C activity in rat vascular smooth muscle.
2001 Jan
Dose-response relationships and pharmacokinetics of vitellogenin in rainbow trout after intravascular administration of 17alpha-ethynylestradiol.
2001 Jan
Evaluation of an EIA method for measuring serum levels of the estrogen metabolite 2-hydroxyestrone in adults.
2001 Jan
Estradiol levels in psychotic disorders.
2001 Jan
Neuroprotection by estradiol.
2001 Jan
Effects of heterocyclic amines with mammary gland carcinogenic potential on estrogenic response of uterus in ovariectomized rats.
2001 Jan 10
Affinity labeling of rat glutathione S-transferase isozyme 1-1 by 17beta -iodoacetoxy-estradiol-3-sulfate.
2001 Jan 19
Reduction of gamma-aminobutyric acid-ergic neurotransmission as a putative mechanism of radiation induced activation of the gonadotropin releasing-hormone-pulse generator leading to precocious puberty in female rats.
2001 Jan 5
Hormone binding by protein disulfide isomerase, a high capacity hormone reservoir of the endoplasmic reticulum.
2001 Jan 5
Acquisition of Lubrol insolubility, a common step for growth hormone and prolactin in the secretory pathway of neuroendocrine cells.
2001 Jan 5
In vivo regulation of syndecan-3 expression in the rat uterus by 17 beta-estradiol.
2001 Jan 5
Glutathione stimulates sulfated estrogen transport by multidrug resistance protein 1.
2001 Mar 2
Estrogen decreases osteoclast formation by down-regulating receptor activator of NF-kappa B ligand (RANKL)-induced JNK activation.
2001 Mar 23
Enhanced multispecificity of arabidopsis vacuolar multidrug resistance-associated protein-type ATP-binding cassette transporter, AtMRP2.
2001 Mar 23
The unusual binding properties of the third distinct teleost estrogen receptor subtype ERbetaa are accompanied by highly conserved amino acid changes in the ligand binding domain.
2004 Jun
Sulfonation of 17beta-estradiol and inhibition of sulfotransferase activity by polychlorobiphenylols and celecoxib in channel catfish, Ictalurus punctatus.
2007 Mar 10
Complex actions of estradiol-3-sulfate in late gestation fetal brain.
2011 Jul
[Study of gonadal hormone drugs in blocking filovirus entry of cells in vitro].
2015 Dec
Evaluation of Effects of Topical Estradiol Benzoate Application on Cutaneous Wound Healing in Ovariectomized Female Mice.
2016
Effects of Exposure to Estradiol Benzoate or Flutamide at the Weaning Age on Expression of Connexins in the Caudal Epididymis of Adult Rat.
2016 Dec
Changes in Expression of Connexin Isoforms in the Caudal Epididymis of Adult Sprague-Dawley Rats exposed to Estradiol Benzoate or Flutamide at the Neonatal Age.
2016 Sep
Patents

Sample Use Guides

In Vitro Use Guide
The influence of estradiol benzoate on the proliferation of bone cells was investigated in vitro. The fibulae from 19-day fetal rats were pulse-labeled with 3H-thymidine after various periods of culture on estrogen-supplemented (5 microgram/ml) or control media. The analysis revealed that the cell division was restricted to osteogenic cells of undifferentiated appearance. No label was found in osteoblasts or in osteoclasts. At the time of explantation, about 30% of osteogenic cells were labeled. However, this percentage varied considerably after different intervals of culture. In the control bones, it decreased during first 12 hours to 15% and then rose slowly to attain a preculture value after 48 hours. In the presence of estradiol, the initial decline of labeled cells was less pronounced. The percentage recovered to a preculture level already after 24 hours and continued to increase thereafter. The numbers of labeled osteogenic cells, in estrogen-treated bones, were significantly higher than in controls already after 12 hours of culture. It is concluded that the fetal rat bones undergo in vitro a period of adaptation to a new environment as indicated by a transient decrease of dividing cells. Estradiol benzoate appears to shorten this period by stimulating the proliferation of undifferentiated cells.
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:35:34 UTC 2021
Edited
by admin
on Fri Jun 25 21:35:34 UTC 2021
Record UNII
4TI98Z838E
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ESTRADIOL
GREEN BOOK   HSDB   INCI   INN   JAN   MI   ORANGE BOOK   USP   VANDF   WHO-DD  
INN   INCI  
Official Name English
VAGIFEM
Brand Name English
ESTRADIOL IMPURITY A [IP]
Common Name English
WC3011
Code English
ESTRADIOL [VANDF]
Common Name English
ETHINYLESTRADIOL IMPURITY D [EP]
Common Name English
ESTRADIOL [WHO-DD]
Common Name English
INNOFEM
Brand Name English
ESTRA-1,3,5(10)-TRIENE-3,17-DIOL (17.BETA.)-
Common Name English
ESTRADIOL BENZOATE SPECIFIED IMPURITY A [EP]
Common Name English
17-.BETA.-OESTRADIOL
Common Name English
DIVIGEL
Brand Name English
ESTRADIOL [ORANGE BOOK]
Common Name English
17BETA-ESTRADIOL
Common Name English
ESTRADIOL COMPONENT OF COMBIPATCH
Common Name English
FEMPATCH
Brand Name English
ESTRADIOL COMPONENT OF CLIMARA PRO
Common Name English
ESTRADIOL [GREEN BOOK]
Common Name English
OESTRADIOL
Common Name English
IMVEXXY
Brand Name English
ESTRADIOL [JAN]
Common Name English
ELESTRIM
Brand Name English
CLIMARA
Brand Name English
NSC-20293
Code English
ALORA
Brand Name English
ORIAHNN COMPONENT ESTRADIOL
Brand Name English
13.BETA.-METHYL-1,3,5(10)-GONATRIENE-3,17.BETA.-OL
Systematic Name English
ESTRADIOL COMPONENT OF BIJUVA
Common Name English
E2
Common Name English
ESTRADIOL [INN]
Common Name English
ESTRADIOL BENZOATE IMPURITY A [EP]
Common Name English
ESCLIM
Brand Name English
ESTRING
Brand Name English
EVAMIST
Brand Name English
ESTRACE
Brand Name English
PREFEST COMPONENT ESTRADIOL
Common Name English
COMBIPATCH COMPONENT ESTRADIOL
Common Name English
ESTRADIOL COMPONENT OF ANGELIQ
Common Name English
BIJUVA COMPONENT ESTRADIOL
Common Name English
ESTROGEL
Brand Name English
NSC-9895
Code English
WC-3011
Code English
ESTRADIOL [HSDB]
Common Name English
ESTRADIOL VALERATE METABOLITE E2
Common Name English
MENOSTAR
Brand Name English
ESTRADIOL COMPONENT OF ACTIVELLA
Common Name English
ESTRADIOL ANHYDROUS
Common Name English
17.BETA.-ESTRADIOL
Common Name English
ESTRADIOL [USP]
Common Name English
ESTRADERM
Brand Name English
3,17.BETA.-DIHYDROXYESTRA-1,3,5(10)-TRIENE
Systematic Name English
GYNODIOL
Brand Name English
ESTRADIOL 17-BETA
VANDF  
Common Name English
ESTRADIOL 17-BETA [VANDF]
Common Name English
ESTRADIOL [MI]
Common Name English
ESTRADIOL [INCI]
Common Name English
CLIMARA PRO COMPONENT ESTRADIOL
Common Name English
ESTRADIOL VALERATE IMPURITY A [EP]
Common Name English
(+)-3,17.BETA.-ESTRADIOL
Systematic Name English
ESTRA-1,3,5(10)-TRIENE-3,17.BETA.-DIOL
Systematic Name English
VIVELLE
Brand Name English
ESTRADIOL COMPONENT OF ORIAHNN
Brand Name English
17-BETA-OESTRADIOL
Common Name English
ANGELIQ COMPONENT ESTRADIOL
Common Name English
ESTRADIOL [USP-RS]
Common Name English
ACTIVELLA COMPONENT ESTRADIOL
Common Name English
ESTRADIOL COMPONENT OF PREFEST
Common Name English
Classification Tree Code System Code
LOINC 35384-7
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
LOINC 34290-7
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LOINC 34286-5
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LOINC 12595-5
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LOINC 2239-2
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WHO-ATC G03CA03
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
WHO-VATC QG03CA03
Created by admin on Fri Jun 25 21:35:36 UTC 2021 , Edited by admin on Fri Jun 25 21:35:36 UTC 2021
CFR 21 CFR 522.840
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
LOINC 83097-6
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LOINC 2240-0
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LOINC 14715-7
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LOINC 15062-3
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LOINC 12214-3
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LOINC 34288-1
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FDA ORPHAN DRUG 231706
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WHO-VATC QG03CA53
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LOINC 25401-1
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CFR 21 CFR 310.527
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WHO-VATC QG03AB08
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NDF-RT N0000011402
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WHO-ATC G03AA14
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LOINC 13883-4
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LOINC 2246-7
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WHO-VATC QG03AA14
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CFR 21 CFR 556.240
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LOINC 72873-3
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LOINC 34287-3
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LOINC 55857-7
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LOINC 35207-0
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LOINC 21263-9
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LIVERTOX 372
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LOINC 2243-4
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LOINC 2245-9
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LOINC 2238-4
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LOINC 31176-1
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WHO-ATC G03CA53
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WHO-ATC G03AB08
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LOINC 14960-9
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LOINC 2241-8
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EMA ASSESSMENT REPORTS IOA (WITHDRAWN: CONTRACEPTION)
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NDF-RT N0000000100
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LOINC 12213-5
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LOINC 34291-5
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CFR 21 CFR 522.2477
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NDF-RT N0000175825
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LOINC 44730-0
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LOINC 34289-9
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CFR 21 CFR 862.1430
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CFR 21 CFR 862.1260
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NCI_THESAURUS C2293
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LOINC 13736-4
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LOINC 55858-5
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LOINC 2242-6
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LOINC 2244-2
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Code System Code Type Description
IUPHAR
1013
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY
ECHA (EC/EINECS)
200-023-8
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY
WIKIPEDIA
ESTRADIOL
Created by admin on Fri Jun 25 21:35:36 UTC 2021 , Edited by admin on Fri Jun 25 21:35:36 UTC 2021
PRIMARY
LACTMED
Estradiol
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY
DRUG BANK
DB00783
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY
EVMPD
SUB96040
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY
MERCK INDEX
M5028
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY Merck Index
MESH
D004958
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY
EPA CompTox
50-28-2
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY
INN
406
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY
NCI_THESAURUS
C478
Created by admin on Fri Jun 25 21:35:36 UTC 2021 , Edited by admin on Fri Jun 25 21:35:36 UTC 2021
PRIMARY
ChEMBL
CHEMBL135
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY
DRUG CENTRAL
1057
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY
CAS
50-28-2
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY
EVMPD
SUB07242MIG
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY
FDA UNII
4TI98Z838E
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY
RXCUI
4083
Created by admin on Fri Jun 25 21:35:36 UTC 2021 , Edited by admin on Fri Jun 25 21:35:36 UTC 2021
PRIMARY RxNorm
EVMPD
SUB21195
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY
HSDB
3589
Created by admin on Fri Jun 25 21:35:35 UTC 2021 , Edited by admin on Fri Jun 25 21:35:35 UTC 2021
PRIMARY
USP_CATALOG
1250008
Created by admin on Fri Jun 25 21:35:36 UTC 2021 , Edited by admin on Fri Jun 25 21:35:36 UTC 2021
PRIMARY USP-RS
PUBCHEM
5757
Created by admin on Fri Jun 25 21:35:36 UTC 2021 , Edited by admin on Fri Jun 25 21:35:36 UTC 2021
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> SUBSTRATE
BINDER->LIGAND
BINDING
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> INHIBITOR
IC50
BASIS OF STRENGTH->SUBSTANCE
ASSAY (HPLC)
USP
TRANSPORTER -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
SUBSTANCE->BASIS OF STRENGTH
BINDER->LIGAND
BINDING
TARGET -> AGONIST
Related Record Type Details
PRODRUG -> METABOLITE ACTIVE
METABOLITE -> PARENT
E2 is then extensively metabolized to estrone (E1) (15%), estrone sulfate (E1S) (65%), and other compounds.
METABOLITE -> PARENT
PRODRUG -> METABOLITE ACTIVE
METABOLITE -> PARENT
METABOLITE -> PARENT
E2 is then extensively metabolized to estrone (E1) (15%), estrone sulfate (E1S) (65%), and other compounds.
METABOLITE LESS ACTIVE -> PARENT
IN-VITRO
PRODRUG -> METABOLITE ACTIVE
PARENT -> METABOLITE ACTIVE
PARENT -> METABOLITE
Metabolite produced by hydrolysis. Estramustine,s primary mechanism of antineoplastic action is inhibition of mitosis.
PLASMA
METABOLITE -> PARENT
IN-VITRO
Scientific Literature
METABOLITE -> PARENT
MAJOR
METABOLITE -> PARENT
METABOLITE -> PARENT
IN-VIVO
URINE
PRODRUG -> METABOLITE ACTIVE
Related Record Type Details
PARENT -> IMPURITY
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
PARENT -> IMPURITY
CHROMATOGRAPHIC PURITY (TLC)
USP
IMPURITY -> PARENT
IMPURITY -> PARENT
PARENT -> IMPURITY
IMPURITY -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC ESTRADIOL VALERATE

Single Dose

Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC ESTRADIOL VALERATE

Single Dose