|
| | Erteberel (LY500307) Basic information |
| Product Name: | Erteberel (LY500307) | | Synonyms: | LY500307;(3aS,4R,9bR)-1,2,3,3a,4,9b-Hexahydro-4-(4-hydroxyphenyl)cyclopenta[c][1]benzopyran-8-ol;Erteberel;LY500307 (Erteberel);(3aS,4R,9bR)-4-(4-hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-ol;Erteberel (LY500307);Phenchlobenpyrrone;CS-897 | | CAS: | 533884-09-2 | | MF: | C18H18O3 | | MW: | 282.33 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 533884-09-2.mol |  |
| | Erteberel (LY500307) Chemical Properties |
| Boiling point | 485.2±45.0 °C(Predicted) | | density | 1.268 | | storage temp. | Store at -20°C | | solubility | insoluble in H2O; ≥14.1 mg/mL in DMSO; ≥48.3 mg/mL in EtOH | | form | solid | | pka | 9.79±0.30(Predicted) |
| | Erteberel (LY500307) Usage And Synthesis |
| Uses | Erteberel is a highly selective estrogen receptor β (ERβ) agonist. | | Biological Activity | 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] | | references | [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. |
| | Erteberel (LY500307) Preparation Products And Raw materials |
|
