Home Endocrinology & Hormones Estrogen/progestogen Receptor agonist Erteberel (LY500307) For research use only.

Erteberel (LY500307)

Synonyms: Erteberel

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

Erteberel (LY500307) Chemical Structure

Erteberel (LY500307) Chemical Structure

CAS No. 533884-09-2

Purity & Quality Control

Erteberel (LY500307) Related Products

Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Signaling Pathway

Biological Activity

Description LY500307 is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.
Features Demonstrates significantly higher binding activity toward ERβ than ERα.
Targets
ERβ [1]
0.66 nM(EC50)
In vitro
In vitro 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. [1]
In Vivo
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]
Animal Research Animal Models CD-1 mice
Dosages 0.01-0.05 mg/kg
Administration Oral gavage daily

Chemical Information & Solubility

Molecular Weight 282.33 Formula

C18H18O3
CAS No. 533884-09-2 SDF Download Erteberel (LY500307) SDF
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 57 mg/mL ( (201.89 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 57 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

Question 1:
If your product S1598 LY500307 is chiral isoform or not?

Answer:
Our S1598 LY500307 is a chiral isoform. The chiral part is from the raw material.

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