Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C18H24O2 |
Molecular Weight | 272.382 |
Optical Activity | ( + ) |
Defined Stereocenters | 5 / 5 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@]3([H])C4=C(CC[C@@]23[H])C=C(O)C=C4
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
Molecular Formula | C18H24O2 |
Molecular Weight | 272.382 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 5 / 5 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/11250930https://pubchem.ncbi.nlm.nih.gov/compound/222757http://www.drugbank.ca/drugs/DB00783Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/020375s027lbl.pdf
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11250930https://pubchem.ncbi.nlm.nih.gov/compound/222757http://www.drugbank.ca/drugs/DB00783
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.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25231731https://books.google.ru/books?id=L4YQ50SbBnsC&pg=PA223&lpg=PA223&dq=estradiol+cross+blood+brain+barrier&source=bl&ots=1XAPNkXVXI&sig=_VCp7qIuyiwBe9cGGJDMvmdR8zg&hl=ru&sa=X&ved=0ahUKEwjjk6vD8r7PAhWCFywKHU3xD8c4ChDoAQg4MAU#v=onepage&q=estradiol%20cross%20blood%20brain%20barrier&f=false, retrieved from
Curator's Comment: Estrogen Effects in Psychiatric Disorders
Niels Bergemann,Anita Riecher-Rössler, p.223
Originator
Sources: http://www.google.ru/patents/US2054271https://books.google.ru/books?id=_J2ti4EkYpkC&pg=PA1478&lpg=PA1478&dq=ESTRADIOL+year+introduced&source=bl&ots=N5lzH8ALwu&sig=V9zqvrxhsCojxBpoWmAWSN7AXcc&hl=ru&sa=X&ved=0ahUKEwj975678L7PAhVGXSwKHb5cBkUQ6AEISDAH#v=onepage&q=ESTRADIOL%20year%20introduced&f=false, retrieved from Pharmaceutical Manufacturing Encyclopedia, 3rd Edition : William Andrew Publishing, p.1475
Curator's Comment: Introduced in 1952
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P08842 Gene ID: 412.0 Gene Symbol: STS Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/11250930 |
|||
Target ID: CHEMBL206 Sources: http://www.drugbank.ca/drugs/DB00783 |
0.0084 nM [EC50] | ||
Target ID: CHEMBL242 Sources: http://www.drugbank.ca/drugs/DB00783 |
1.4 nM [EC50] | ||
Target ID: CHEMBL1871 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16309907 |
19.1 nM [IC50] | ||
Target ID: CHEMBL206 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/222757 |
0.13 nM [Ki] | ||
Target ID: CHEMBL242 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/222757 |
0.09 nM [Kd] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | CLIMARA Approved UseClimara 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 Date1974 |
|||
Preventing | CLIMARA Approved UseClimara 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 Date1974 |
|||
Primary | CLIMARA Approved UseClimara 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 Date1974 |
|||
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: - |
yes | |||
Sources: https://pubs.acs.org/doi/abs/10.1021/mp900077q Page: - |
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: - |
minor | |||
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minor | |||
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minor | |||
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no | |||
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no | |||
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no | |||
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no | |||
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no | |||
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yes [Km 7 uM] | |||
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yes | |||
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yes | |||
Sources: https://www.pnas.org/content/93/18/9776.short Page: - |
yes | |||
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yes | |||
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yes | |||
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yes | |||
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yes | |||
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yes |
PubMed
Title | Date | PubMed |
---|---|---|
Effect of estradiol benzoate on the proliferation of osteogenic cells in fetal rat fibulae cultured in vitro. | 1978 Mar |
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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 |
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Sulfation of estrone and 17 beta-estradiol in human liver. Catalysis by thermostable phenol sulfotransferase and by dehydroepiandrosterone sulfotransferase. | 1992 May-Jun |
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Growth stimulation of a rat pituitary cell line MtT/E-2 by environmental estrogens in vitro and in vivo. | 1999 Aug |
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Sex steroids and odorants modulate gonadotropin-releasing hormone secretion in primary cultures of human olfactory cells. | 1999 Nov |
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Perinatal exposure to estrogenic compounds and the subsequent effects on the prostate of the adult rat: evaluation of inflammation in the ventral and lateral lobes. | 1999 Nov-Dec |
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Estrogen and aryl hydrocarbon receptor expression and crosstalk in human Ishikawa endometrial cancer cells. | 2000 Apr |
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Effect of chlorinated hydrocarbons on expression of cytochrome P450 1A1, 1A2 and 1B1 and 2- and 4-hydroxylation of 17beta-estradiol in female Sprague-Dawley rats. | 2000 Aug |
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Proteinase inhibitor 9, an inhibitor of granzyme B-mediated apoptosis, is a primary estrogen-inducible gene in human liver cells. | 2000 Feb 25 |
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The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution. | 2000 Jan |
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The aryl hydrocarbon receptor interacts with estrogen receptor alpha and orphan receptors COUP-TFI and ERRalpha1. | 2000 Jan 1 |
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Atheroprotective effect of estriol and estrone sulfate on human vascular smooth muscle cells. | 2000 Jan-Feb |
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Crosstalk between estrogen receptor alpha and the aryl hydrocarbon receptor in breast cancer cells involves unidirectional activation of proteasomes. | 2000 Jul 28 |
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Six high-priority organochlorine pesticides, either singly or in combination, are nonestrogenic in transfected HeLa cells. | 2000 Mar-Apr |
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Estradiol acts as a germ cell survival factor in the human testis in vitro. | 2000 May |
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Assaying estrogenicity by quantitating the expression levels of endogenous estrogen-regulated genes. | 2000 May |
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Estrogen activation of the nuclear orphan receptor CAR (constitutive active receptor) in induction of the mouse Cyp2b10 gene. | 2000 Nov |
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Female sex steroids: effects upon microglial cell activation. | 2000 Nov 1 |
|
Changes in serum and tissue zinc levels in sex hormone-induced prostatic carcinogenesis in the noble rat. | 2000 Nov-Dec |
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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 |
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Effects of arsenite on estrogen receptor-alpha expression and activity in MCF-7 breast cancer cells. | 2000 Oct |
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Antiestrogenic effects of 2,3,7,8-tetrachlorodibenzo-p-dioxin in mouse uterus: critical role of the aryl hydrocarbon receptor in stromal tissue. | 2000 Oct |
|
Repression of chick multidrug resistance-associated protein 1 (chMRP1) gene expression by estrogen. | 2000 Oct 31 |
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Constitutive expression of the steroid sulfatase gene supports the growth of MCF-7 human breast cancer cells in vitro and in vivo. | 2001 Apr |
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Unique protein determinants of the subtype-selective ligand responses of the estrogen receptors (ERalpha and ERbeta ) at AP-1 sites. | 2001 Feb 9 |
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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 |
|
Increased expression of a novel heat shock protein transcript in the mouse uterus during decidualization and in response to progesterone. | 2001 Jan |
|
Follicle selection in cattle: role of luteinizing hormone. | 2001 Jan |
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Lysyl oxidase and MMP-2 expression in dehydroepiandrosterone-induced polycystic ovary in rats. | 2001 Jan |
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Changes in follicle-stimulating hormone and follicle populations during the ovarian cycle of the common marmoset. | 2001 Jan |
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Estradiol-induced attenuation of pulmonary hypertension is not associated with altered eNOS expression. | 2001 Jan |
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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 |
|
Sex steroid hormones enhance immune function in male and female Siberian hamsters. | 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 |
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Dose-response relationships and pharmacokinetics of vitellogenin in rainbow trout after intravascular administration of 17alpha-ethynylestradiol. | 2001 Jan |
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Estradiol levels in psychotic disorders. | 2001 Jan |
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Neuroprotection by estradiol. | 2001 Jan |
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Affinity labeling of rat glutathione S-transferase isozyme 1-1 by 17beta -iodoacetoxy-estradiol-3-sulfate. | 2001 Jan 19 |
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Hormone binding by protein disulfide isomerase, a high capacity hormone reservoir of the endoplasmic reticulum. | 2001 Jan 5 |
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Acquisition of Lubrol insolubility, a common step for growth hormone and prolactin in the secretory pathway of neuroendocrine cells. | 2001 Jan 5 |
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In vivo regulation of syndecan-3 expression in the rat uterus by 17 beta-estradiol. | 2001 Jan 5 |
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Glutathione stimulates sulfated estrogen transport by multidrug resistance protein 1. | 2001 Mar 2 |
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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 Vivo Use Guide
Curator's Comment: Estradiol benzoate is not approved by the FDA for use in humans in the United States.
Unknown
Route of Administration:
Unknown
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21273638
Estradiol-3-sulfate (E2SO4) infused intracerebroventricularly (icv) significantly increased plasma adrenocorticotropic hormone (ACTH) and cortisol concentrations. All minipumps in the treated fetuses were filled with E2SO4 in the vehicle (water) and minipumps in the control fetuses were filled with vehicle only. These minipumps deliver a constant infusion of 5 μL/h; the concentration of E2SO4 in infusates was therefore 8.33 μg/μL. It was concluded, that E2SO4 had complex actions on the fetal brain, which might involve deconjugation by steroid sulfatase. But that the net result of direct E2SO4 icv infusion was more complex than could be accounted for by infusion of E2 alone.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:14:36 GMT 2023
by
admin
on
Fri Dec 15 15:14:36 GMT 2023
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Record UNII |
4TI98Z838E
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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LOINC |
35384-7
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34290-7
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2239-2
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WHO-ATC |
G03CA03
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WHO-VATC |
QG03CA03
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CFR |
21 CFR 522.840
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LOINC |
83097-6
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12214-3
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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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G03AA14
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13883-4
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2246-7
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WHO-VATC |
QG03AA14
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CFR |
21 CFR 556.240
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72873-3
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LIVERTOX |
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EMA ASSESSMENT REPORTS |
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NDF-RT |
N0000000100
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admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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LOINC |
12213-5
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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LOINC |
34291-5
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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CFR |
21 CFR 522.2477
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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NDF-RT |
N0000175825
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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LOINC |
44730-0
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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LOINC |
34289-9
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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CFR |
21 CFR 862.1430
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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CFR |
21 CFR 862.1260
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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NCI_THESAURUS |
C2293
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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LOINC |
13736-4
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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LOINC |
55858-5
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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LOINC |
83096-8
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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LOINC |
2242-6
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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LOINC |
2244-2
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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Code System | Code | Type | Description | ||
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1013
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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200-023-8
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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ESTRADIOL
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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Estradiol
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admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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DB00783
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admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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SUB96040
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admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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23965
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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m5028
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | Merck Index | ||
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Estradiol (medication)
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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D004958
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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20293
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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DTXSID0020573
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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406
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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C478
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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CHEMBL135
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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1057
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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50-28-2
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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100000091739
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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9895
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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4TI98Z838E
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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16469
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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1250008
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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SUB07242MIG
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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4TI98Z838E
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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4083
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | RxNorm | ||
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SUB21195
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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3589
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY | |||
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5757
Created by
admin on Fri Dec 15 15:14:37 GMT 2023 , Edited by admin on Fri Dec 15 15:14:37 GMT 2023
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PRIMARY |
Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT | |||
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BINDER->LIGAND |
BINDING
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SALT/SOLVATE -> PARENT |
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METABOLIC ENZYME -> SUBSTRATE | |||
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TARGET -> INHIBITOR |
BINDING
IC50
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SOLVATE->ANHYDROUS | |||
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METABOLIC ENZYME -> INHIBITOR |
IC50
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
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TRANSPORTER -> INHIBITOR | |||
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TARGET -> AGONIST |
BINDING
IC50
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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SUBSTANCE->BASIS OF STRENGTH |
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BINDER->LIGAND |
BINDING
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TARGET -> AGONIST |
Binding Assay
IC50
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Related Record | Type | Details | ||
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PRODRUG -> METABOLITE ACTIVE | |||
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METABOLITE -> PARENT |
E2 is then extensively metabolized to estrone (E1) (15%), estrone sulfate (E1S) (65%), and other compounds.
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METABOLITE -> PARENT |
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PRODRUG -> METABOLITE ACTIVE |
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PRODRUG -> METABOLITE ACTIVE |
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METABOLITE -> PARENT |
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METABOLITE -> PARENT |
E2 is then extensively metabolized to estrone (E1) (15%), estrone sulfate (E1S) (65%), and other compounds.
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METABOLITE LESS ACTIVE -> PARENT |
IN-VITRO
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PRODRUG -> METABOLITE ACTIVE | |||
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PRODRUG -> METABOLITE ACTIVE | |||
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METABOLITE -> PARENT |
IN-VIVO
URINE
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PARENT -> METABOLITE |
Metabolite produced by hydrolysis. Estramustine,s primary mechanism of antineoplastic action is inhibition of mitosis.
PLASMA
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METABOLITE -> PARENT |
MAJOR
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PARENT -> METABOLITE ACTIVE | |||
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METABOLITE -> PARENT |
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METABOLITE -> PARENT |
IN-VITRO
Scientific Literature
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PRODRUG -> METABOLITE ACTIVE |
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Related Record | Type | Details | ||
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PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (TLC)
USP
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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PARENT -> IMPURITY |
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IMPURITY -> PARENT |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Tmax | PHARMACOKINETIC |
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ESTRADIOL VALERATE |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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ESTRADIOL VALERATE |
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