Erteberel (LY500307)

Erteberel (LY500307)

Catalog Number:
L002370058APE
Mfr. No.:
APE-B1518
Price:
$528
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      • Overview
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          Background

          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]

      • Properties
        • Categories
          ERβ agonist, potent and selective
          Alternative Name
          (3aS,4R,9bR)-4-(4-hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-ol
          CAS Number
          533884-09-2
          Molecular Formula
          C18H18O3
          Molecular Weight
          282.33
          Appearance
          A solid
          Purity
          98.21%
          Solubility
          insoluble in H2O; ≥14.1 mg/mL in DMSO; ≥48.3 mg/mL in EtOH
          Storage
          Store at -20°C
          SMILES
          C1CC2C(C1)C3=C(C=CC(=C3)O)OC2C4=CC=C(C=C4)O

          * For Research Use Only

      • Reference
        • 1. Gangadhara R. Sareddy, Uday P. Pratap, et al. "Activation of estrogen receptor beta signaling reduces stemness of glioma stem cells." Stem Cells. 2021 May;39(5):536-550. PMID:33470499

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