EGX358
EGX358 is a selective, orally active estrogen receptor β (ERβ) agonist with an EC50 of 27.4 nM for ERβ. EGX358 enhances object recognition ability, spatial memory and memory consolidation, and attenuates drug-induced vasomotor responses. EGX358 alleviates partial uterine atrophy without inducing uterine hypertrophy, while it does not alter anxiety-like behavior, depression-like behavior or body weight. EGX358 can be used in research related to Alzheimer's disease and menopause.
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- CAS No.: 2245952-60-5
- Formule: C13H18O2
- Masse moléculaire:206.28
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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ERβ 27.4 nM (EC50) |
EGX358 potently activates ERβ with an EC50 of 27.4 nM, and exhibits 750-fold selectivity for ERβ over ERα[1].
EGX358 shows 750-fold higher selectivity for ERβ than for ERα, and exhibits no off-target activity against a panel of other nuclear receptors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
EGX358 (oral administration; once daily; for 64 consecutive days) reduces senktide-induced elevation of tail skin temperature in ovariectomized mice, enhances their spatial recognition and object recognition memory, without altering body weight, anxiety-like or depression-like behaviors of the mice, nor affecting the expression/phosphorylation levels of brain proteins[3].
EGX358 (10 mg/kg; p.o.; once daily; for 8 weeks) significantly enhances object recognition memory in ovariectomized EFAD mouse models of Alzheimer's disease[4].
EGX358 (0.5 mg/kg; p.o.; once daily; for 64 days) reduces senktide-induced vasodilation, improves spatial recognition memory and object recognition memory in young ovariectomized mice, and exerts no adverse effects on mouse body weight, anxiety-like behavior or depression-like behavior[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:APOE-TR+/+/5xFAD+/− (EFAD) (female, ovariectomized at 5 months of age; homozygous for human APOE3 (E3FAD) or heterozygous for human APOE3 and APOE4 (E3/4FAD))[1]
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Dosage:10 mg/kg
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Administration:p.o.; daily; 8 weeks
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Result:Enhanced object recognition memory in both genotypes but did not improve object placement memory.
Reduced tail-skin temperature elevation in E3FAD mice but not in E3/4FAD mice.
Did not affect anxiety-like behavior or body weight; slightly increased uterine weight without causing hypertrophy.
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Animal Model:C57BL/6 (8-week-old female, bilaterally ovariectomized, senktide injection to model hot flash-like vasodilation)[2]
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Dosage:0.5 mg/kg
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Administration:p.o.; daily; 64 days
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Result:Enhanced object placement and object recognition memory.
Did not significantly affect anxiety-like behavior, depression-like behavior or body-weight gain.
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Animal Model:APOE-TR+/+/5xFAD+/− (EFAD) (female, ovariectomized at 5 months of age)[4]
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Dosage:10 mg/kg
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Administration:p.o.; daily; 8 weeks
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Result:Significantly enhanced object recognition memory in both E3FAD and E3/4FAD mice.
Did not affect object placement memory, anxiety-like behaviors in the open field or elevated plus maze, or vasomotor symptoms.
Chemical Information
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CAS No. 2245952-60-5
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Masse moléculaire 206.28
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Formule C13H18O2
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SMILES
OC[C@@H]1CC[C@@H](C2=CC=C(C=C2)O)CC1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Schwabe MR, et al. The novel estrogen receptor beta agonist EGX358 and genotype influence memory, vasomotor, and anxiety outcomes in an Alzheimer's mouse model. Frontiers in aging neuroscience. 2024;16:1477045. [Content Brief]
[2]. Fleischer AW, et al. Long-term oral administration of a novel estrogen receptor beta agonist enhances memory and alleviates drug-induced vasodilation in young ovariectomized mice. Hormones and behavior. 2021 Apr;130:104948. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGX358 Related Classifications
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