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research use only
Cat.No.S2466
| Related Targets | Adrenergic Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR |
|---|---|
| Other Estrogen/progestogen Receptor Products | Elacestrant (RAD1901) Dihydrochloride Vepdegestrant (ARV471) MPP dihydrochloride Cholesterol Endoxifen HCl G15 Chrysin Licochalcone A AZD9496 PHTPP |
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In vitro |
DMSO
: 57 mg/mL
(197.64 mM)
Ethanol : 10 mg/mL Water : Insoluble |
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In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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| Molecular Weight | 288.39 | Formula | C18H24O3 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 50-27-1 | Download SDF | Storage of Stock Solutions |
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| Synonyms | NSC-12169 | Smiles | CC12CCC3C(C1CC(C2O)O)CCC4=C3C=CC(=C4)O | ||
| Targets/IC50/Ki |
ER
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|---|---|
| In vitro |
MTT assays using G-1 shows that, in SkBr3 cells, the proliferative effect induced by 100 nM G-1 is abolished in the presence of 1 μM estriol which acts as an antagonist of GPR30-dependent pathway.
A cell-free transcription assay demonstrates that the antiestrogenic activity exhibited by estriol is because of interferring with estradiol-induced positive cooperative binding and receptor dimerization, binding of hER complexes to ERE, as well as reducing estradiol-dependent transcription in a dose-dependent manner.
A recent study shows that estrogen (estrone, estradiol, and estriol) inhibits Alzheimer's disease-associated low-order Aβ oligomer formation, and among them, estriol shows the strongest in vitro activity.
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| In vivo |
In mPTEN+/- mice, estriol treatments resulted in a 187.54% gain in the relative ratio of uterine wet weight to body weight; estriol also increases the ratio to 176.88% in wild-type mice.
Estriol treatment (20 mg/kg ip), in vivo, sensitizes Kupffer cells to LPS via mechanisms dependent on an increase in CD14 by elevated portal blood endotoxin caused by increased gut permeability in rats; while one-half of the rats given estriol intraperitoneally 24 hours before an injection of a sublethal dose of LPS (5 mg/kg) died within 24 hours.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05000424 | Unknown status | Quality of Life|Pregnancy Related |
Franklin Health Research |
November 1 2021 | Not Applicable |
| NCT05012072 | Recruiting | Mental Health Wellness 1|Preterm Birth |
Microgen LLC |
August 1 2021 | Phase 2 |
| NCT04305093 | Completed | Obesity; Endocrine|Hormone Disturbance |
Precision Analytical Inc. |
December 15 2019 | -- |
| NCT04267731 | Completed | Aging Well |
Vemico Ltd.|University of Roehampton |
December 1 2019 | Not Applicable |
| NCT03116022 | Unknown status | Dyspareunia|Menopause|Sexual Dysfunction |
University of Sao Paulo |
June 1 2017 | Phase 1 |
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