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Erteberel (LY500307)ERβ agonist, potent and selective

Erteberel (LY500307)

Catalog No. B1518
Size Price Stock Qty
10mM (in 1mL DMSO) $140.00 In stock
5mg $119.00 In stock
10mg $224.00 In stock
50mg $679.00 In stock
200mg $1,729.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Erteberel (LY500307)

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Chemical Properties

Cas No. 533884-09-2 SDF Download SDF
Chemical Name (3aS,4R,9bR)-4-(4-hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-ol
Canonical SMILES C1CC2C(C1)C3=C(C=CC(=C3)O)OC2C4=CC=C(C=C4)O
Formula C18H18O3 M.Wt 282.33
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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]

Reference:
[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.