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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 2245952-60-5
- 화학식: C13H18O2
- 분자량:206.28
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
Biological Activity
|
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.
-
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]
-
Dosage:10 mg/kg
-
Administration:p.o.; daily; 8 weeks
-
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.
-
Animal Model:C57BL/6 (8-week-old female, bilaterally ovariectomized, senktide injection to model hot flash-like vasodilation)[2]
-
Dosage:0.5 mg/kg
-
Administration:p.o.; daily; 64 days
-
Result:Enhanced object placement and object recognition memory.
Did not significantly affect anxiety-like behavior, depression-like behavior or body-weight gain.
-
Animal Model:APOE-TR+/+/5xFAD+/− (EFAD) (female, ovariectomized at 5 months of age)[4]
-
Dosage:10 mg/kg
-
Administration:p.o.; daily; 8 weeks
-
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
-
CAS No. 2245952-60-5
-
분자량 206.28
-
화학식 C13H18O2
-
SMILES
OC[C@@H]1CC[C@@H](C2=CC=C(C=C2)O)CC1
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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)
EGX358 Related Classifications
HY-186284 Related Classifications
Powered by Bioz