Erteberel

Erteberel is an estrogen receptor beta (ERbeta) agonist. It is selective for ERbeta over ERalpha in reporter assays using PC3 cells expressing the human receptors (EC50s = 0.66 and 19.4 nM, respectively). Ertebrel (5 µM) induces apoptosis and cell cycle arrest at the G2/M phase in U87MG and U251 glioblastoma cells. It enhances cytotoxicity induced by cisplatin (Cay-13119), lomustine (Cay-21237), or bleomycin (Cay-13877) in U251 cells when used at a concentration of 1 µM. Ertebrel (5 mg/kg) reduces tumor growth in a U251 orthotopic model of glioblastoma in ovariectomized mice. It decreases prostate weight but does not affect serum testosterone or dihydrotestosterone levels in a mouse model of benign prostatic hyperplasia (BPH) when administered at doses of 0.01, 0.025, and 0.05 mg/kg.Formal Name: (3aS,4R,9bR)-1,2,3,3a,4,9b-hexahydro-4-(4-hydroxyphenyl)-cyclopenta[c][1]benzopyran-8-ol. CAS Number: 533884-09-2. Synonyms: LY500307. Molecular Formula: C18H18O3. Formula Weight: 282.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml. lambdamax: 225 nm. SMILES: OC1=CC2=C(C=C1)O[C@@H](C3=CC=C(O)C=C3)[C@]4([H])[C@@]2([H])CCC4. InChi Code: 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. InChi Key: XIESSJVMWNJCGZ-VKJFTORMSA-N.