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.
For research use only. We do not sell to patients.
- CAS No.: 2245952-60-5
- Formula: C13H18O2
- Molecular Weight:206.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
ERβ 27.4 nM (EC50) |
In Vitro
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. Further protocols information, click here.
In Vivo
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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Molecular Weight 206.28
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Formula C13H18O2
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SMILES
OC[C@@H]1CC[C@@H](C2=CC=C(C=C2)O)CC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Protocol for Open Field Test (OF)
The Open Field Test is a rodent behavioral assay that measures spontaneous locomotion, exploratory behavior, and anxiety-like behavior when an animal is placed in a novel open arena. The main readouts are total distance traveled, movement time, velocity, center-zone entries, center-zone time, peripheral-zone time, and thigmotaxis. The assay is based on the conflict between exploration of a novel environment and avoidance of exposed open areas; higher center exploration is commonly interpreted as lower anxiety-like behavior, whereas increased wall-following or peripheral occupancy is interpreted as higher anxiety-like behavior.
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Protocol for Elevated Plus Maze Test
The Elevated Plus Maze is a rodent anxiety-like behavior assay based on the conflict between spontaneous exploration and avoidance of open, elevated, exposed spaces. The apparatus contains two open arms and two closed arms arranged in a plus shape, and rodents normally spend more time in closed arms than open arms. The assay readout is generated by recording arm entries, time spent in open and closed arms, and related exploratory behaviors. Increased open-arm time or open-arm entries is commonly interpreted as reduced anxiety-like behavior, whereas reduced open-arm exploration is interpreted as increased anxiety-like behavior.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Protocol for Tail Suspension Test (TST)
The Tail Suspension Test is a mouse behavioral assay in which an animal is suspended by the tail in an inescapable position, causing alternating escape-directed activity and immobility; the main readout is immobility time, and antidepressant-like treatments generally reduce immobility compared with vehicle controls. The assay detects behavioral response to acute inescapable stress rather than a molecular event; immobility is interpreted as passive stress-coping behavior, while reduced immobility is used as a predictive screen for antidepressant-like activity, with important limitations related to strain, locomotor activity, and tail-climbing behavior.
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Protocol for Water Maze
The Morris Water Maze is a rodent spatial learning and memory assay in which a mouse or rat swims in opaque water to find an escape platform; in the hidden-platform version, the animal cannot see the platform and must use distal extra-maze cues to learn its fixed spatial location. The assay primarily measures hippocampus-dependent spatial learning during acquisition trials and spatial reference memory during probe trials after platform removal; readouts include escape latency, swim path length, swim speed, quadrant occupancy, platform-site crossings, and proximity to the former platform location.
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Protocol for Forced Swim Test (FST)
The Forced Swim Test is a rodent behavioral assay in which a mouse or rat is placed in an inescapable cylinder of water, and the main readout is the time spent immobile versus active escape-related behaviors such as swimming or climbing. Reduced immobility after treatment has historically been interpreted as antidepressant-like activity, but the assay should be interpreted as a behavioral response to acute inescapable stress rather than a complete model of human depression.
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Protocol for Sucrose Preference Test (SPT)
The Sucrose Preference Test is a rodent two-bottle choice assay used to estimate reward-related behavior by measuring preference for a sweet sucrose solution over water. Reduced sucrose preference is commonly interpreted as an anhedonia-like phenotype in stress-based depression models, but it can also be affected by thirst, hunger, body weight, learning, motivation, and general fluid intake.
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
References
[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)