Erteberel (LY500307) Chemical Properties

Boiling point:

485.2±45.0 °C(Predicted)

Density 

1.268

storage temp. 

Store at -20°C

solubility 

insoluble in H2O; ≥14.1 mg/mL in DMSO; ≥48.3 mg/mL in EtOH

form 

solid

pka

9.79±0.30(Predicted)

color 

Off-white to light brown

Erteberel (LY500307) Usage And Synthesis

Uses

Erteberel is a highly selective estrogen receptor β (ERβ) agonist.

Biological Activity

erteberel (ly500307) is a potent and selective erβ (estrogen receptor beta) agonist (ec50 = 0.66 nm). [1]estrogen receptors are nuclear hormone receptors that act as a ligand-activated transcription factor. it regulates gene expression, cell proliferation and differentiation in target tissues and involved in breast cancer, endometrial cancer and osteoporosis etc. [1]in transcription assay of cotransfected human prostate cancer cell line, erteberel showed potency (ec50 = 0.66 nm), selectivity (32-fold) and full agonist function (>90% relative efficacy) to erβ than to erα. [1]in mouse model, prostate wet weight of cd-1 mice were measured following oral daily doses of erteberel for 7 days. results showed reduction on prostate weight in a dose-dependent manner (0.01 mg/kg – 0.05 mg/kg), and no effect on testes/seminal vesicle weight and androgens testosterone/dihydrotestosterone circulating level. [1]

References

[1] norman bh, dodge ja, richardson ti, borromeo ps, lugar cw, jones sa, chen k, wang y, durst gl, barr rj, montrose-rafizadeh c, osborne he, amos rm, guo s, boodhoo a, krishnan v. benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia. j med chem. 2006 oct 19;49(21):6155-7.

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