LY500307 (Erteberel)

LY500307 (Erteberel)

参考价:¥1298
供货周期: 一周
品牌:
规格: 2mg
货号: K1333
CAS号: 533884-09-2
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Information
SKU:K1333   M. Wt:282.33  
Formula:C18H18O3   Solubility:No  
Purity:>99%   Storage:2 years at -20 degrees centigrade  
CAS No.:533884-09-2   Synonyms:N/A  
Chemical NameN/A
Biological Activity
Description LY500307 (Erteberel)
Targets Estrogen receptor beta        
IC50 0.66 nM [EC50]        
In vitro LY500307 can potently inhibit ER-alpha and ER-beta with Ki of 2.68 nM and 0.19 nM. LY500307 shows 14-fold binding selectivity for the beta isoform. LY500307/ER-alpha and LY500307/ER-beta X-ray cocrystal structures show significant differences in the manner in which LY500307 binds within the binding pockets. [1]
In vivo Oral administration of LY500307 (0.01-0.05 mg/kg) in CD-1 mice produces the reduction on prostate weights in a dose-response manner, has no effect on testes and SV weights in this dose range and no effect on T and DHT levels at up to 10% the minimum efficacy dose (0.1 mg/kg), while the nonselective ER agonist diethylstilbestrol (DES) shows significant regression of prostate, testes, and SV and also lowering T and DHT. [1]
Clinical Trials N/A
Features N/A

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