research use only
Cat.No.S2450
| Related Targets | Adrenergic Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR |
|---|---|
| Other Estrogen/progestogen Receptor Inhibitors | Elacestrant (RAD1901) Dihydrochloride MPP dihydrochloride Cholesterol Endoxifen HCl G15 Chrysin Licochalcone A AZD9496 PHTPP Liquiritigenin |
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In vitro |
DMSO
: 48 mg/mL
(198.12 mM)
Ethanol : 48 mg/mL Water : Insoluble |
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In vivo |
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Working concentration: mg/ml;
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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.
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| Molecular Weight | 242.27 | Formula | C15H14O3 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 531-95-3 | Download SDF | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | C1C(COC2=C1C=CC(=C2)O)C3=CC=C(C=C3)O | ||
| Features |
A chiral molecule that can exist as the enantiomers R-equol and S-equol.
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| Targets/IC50/Ki |
ERβ
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| In vitro |
Equol is a metabolite produced from the soy phytoestrogen daidzein by the action of gut microflora. This compound has higher affinity for both ERs (estrogen receptors including ERalpha and ERbeta). It exists as the enantiomers R-equol and S-equol. S-equol has a high binding affinity, preferential for ERbeta with a Ki of 16 nM whereas R-equol binds more weakly and with a preference for ERalpha K with a Ki of 50 nM. This metabolite is superior to all other isoflavones in its antioxidant activity. It has antioestrogenic properties. This compound is a 100-fold more potent than daidzein in stimulating an oestrogenic response. It is also more effective than daidzein in competing with 3 H-oestradiol for binding to the ER. This chemical stimulates the growth of MCF-7 cells in a concentration-dependent manner. Although it exhibits oestrogenic activity, exposure of MCF-7 cells to this compound simultaneously with oestradiol is effective in reducing pS2 mRNA expression. It results in the downregulation of ER mRNA expression.
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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 |
|---|---|---|---|---|---|
| NCT06133101 | Recruiting | Non-Alcoholic Fatty Liver Disease |
Marialena Mouzaki|Children''s Hospital Medical Center Cincinnati |
January 15 2024 | Phase 2 |
| NCT06398236 | Recruiting | Menopause |
Nutrition & Sante Iberia|Adknoma Health Research |
March 17 2023 | Not Applicable |
| NCT01982578 | Completed | Alzheimer''s Disease |
Fundación para la Investigación del Hospital Clínico de Valencia|University of Valencia |
September 1 2017 | Not Applicable |
| NCT03101085 | Completed | Alzheimer Disease |
Russell Swerdlow|Ausio Pharmaceuticals LLC|University of Kansas Medical Center |
May 5 2017 | Phase 1|Phase 2 |
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