533884-09-2 Usage
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.
Check Digit Verification of cas no
The CAS Registry Mumber 533884-09-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 5,3,3,8,8 and 4 respectively; the second part has 2 digits, 0 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 533884-09:
(8*5)+(7*3)+(6*3)+(5*8)+(4*8)+(3*4)+(2*0)+(1*9)=172
172 % 10 = 2
So 533884-09-2 is a valid CAS Registry Number.
533884-09-2Relevant articles and documents
Acid-Promoted Cascade Cyclization to Produce 2-(4′-Alkoxyaryl)-3,4-Fused Tricyclic Dihydrobenzopyrans via a Vinylidene para-Quinone Methide Intermediate
Choi, Dongil,Shiga, Naoki,Franzén, Robert,Nemoto, Tetsuhiro
supporting information, p. 1785 - 1788 (2018/04/27)
We developed a novel method for synthesizing 2-(4-hydroxyaryl)-3,4-fused tricyclic dihydrobenzopyrans with 2,3-syn and 3,4-syn motif based on the acid-promoted cascade cyclization via vinylidene para-quinone methide intermediates. Using easily prepared li
Benzopyrans as selective estrogen receptor β agonists (SERBAs). Part 2: Structure-activity relationship studies on the benzopyran scaffold
Richardson, Timothy I.,Norman, Bryan H.,Lugar, Charles W.,Jones, Scott A.,Wang, Yong,Durbin, Jim D.,Krishnan, Venkatesh,Dodge, Jeffrey A.
, p. 3570 - 3574 (2008/02/04)
Benzopyrans are selective estrogen receptor (ER) β agonists (SERBAs), which bind the ER subtypes α and β in opposite orientations. Here we describe structure-activity relationship studies that led to the discovery of bezopyran 5b. X-ray crystal structures
