Erteberel (LY500307)

ERβ agonist, potent and selective CAS# 533884-09-2

Erteberel (LY500307)

Catalog No. BCC4491----Order now to get a substantial discount!

Product Name & Size Price Stock
Erteberel (LY500307): 5mg $138 In Stock
Erteberel (LY500307): 10mg Please Inquire In Stock
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Chemical structure

Erteberel (LY500307)

3D structure

Chemical Properties of Erteberel (LY500307)

Cas No. 533884-09-2 SDF Download SDF
PubChem ID 10286159 Appearance Powder
Formula C18H18O3 M.Wt 282.33
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 30 mg/mL (106.26 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name (3aS,4R,9bR)-4-(4-hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-ol
SMILES C1CC2C(C1)C3=C(C=CC(=C3)O)OC2C4=CC=C(C=C4)O
Standard InChIKey XIESSJVMWNJCGZ-VKJFTORMSA-N
Standard InChI InChI=1S/C18H18O3/c19-12-6-4-11(5-7-12)18-15-3-1-2-14(15)16-10-13(20)8-9-17(16)21-18/h4-10,14-15,18-20H,1-3H2/t14-,15+,18+/m1/s1
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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Erteberel (LY500307) Dilution Calculator

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Erteberel (LY500307) Molarity Calculator

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Preparing Stock Solutions of Erteberel (LY500307)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.542 mL 17.7098 mL 35.4195 mL 70.8391 mL 88.5489 mL
5 mM 0.7084 mL 3.542 mL 7.0839 mL 14.1678 mL 17.7098 mL
10 mM 0.3542 mL 1.771 mL 3.542 mL 7.0839 mL 8.8549 mL
50 mM 0.0708 mL 0.3542 mL 0.7084 mL 1.4168 mL 1.771 mL
100 mM 0.0354 mL 0.1771 mL 0.3542 mL 0.7084 mL 0.8855 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Erteberel (LY500307)

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. 

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Description

Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. Anti-tumor activities.

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