Erteberel (LY500307)ERβ agonist, potent and selective CAS# 533884-09-2 |
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Quality Control & MSDS
3D structure
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| 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. |
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| 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. |
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| 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
Erteberel (LY500307) Molarity Calculator
| 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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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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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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