Erteberel (LY500307) 533884-09-2

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Molecular Weight:

282.33 LY500307 is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.

Biological Activity

LY500307 shows potent binding affinity for both ERα (Ki 2.68 nM) and ERβ (Ki 0.19 nM), which exhibits 14-fold binding selectivity for the β isoform,
generated using 3H-estradiol and recombinant, full-length, human ERs in
a competitive binding assay. LY500307 shows full agonist function in
both ERα and ERβ assays (>90% relative efficacy), displays potent
inhibition toward ERβ with EC50 of 0.66 nM exhibiting 32 fold
specificity for ERβ than for ERα which has EC50 of 19.4 nM measured
using a transcription assay in the cotransfected human prostate cancer
PC3/ER (α or β)-ERE cell line.


LY500307/ERα and LY500307/ERβ X-ray
cocrystal structures show significant differences in the manner in which
LY500307 binds within the binding pockets. LY500307 displays a
different orientation corresponding to a (ca. 180°) rotation on its
bisphenol axis, and the A ring phenol of LY500307, while bound to
histidine in both structures, locates to different sides of the
imidazole functionality for this interaction explaining the observed
selectivity of LY500307 for ERβ.


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.

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Product Categories : Endocrinology & Hormones > Estrogen/progestogen Receptor Inhibitor