ERβ Agonist

DPN (Diarylpropionitrile) is a non-steroidal estrogen receptor β (ERβ) selective ligand, with an EC₅₀ of 0.85 nM. DPN has neuroprotective effects in a number of neurological diseases.

Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC₅₀s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis.

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

WAY-200070 is a selective estrogen receptor β (ERβ) agonist with an IC₅₀ of 2.3 nM.

Hexestrol is a nonsteroidal synthetic estrogen, with a K_i of 0.06 and 0.06 nM for estrogen receptor alpha (ERα) and ERβ. Hexestrol can be used for the research of the diseases caused by estrogen deficiencym, and it also can increase the weight of cattle.

AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC₅₀s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender selective neuroprotective effects in a male rat model of Parkinson's disease.

WAY-166818 (WAY-818) is a synthetic nonsteroidal estrogen that is a selective agonist of ERβ.

FERb 033 is a selective and potent ERβ agonist (K_i=7.1 nM, EC₅₀=4.8 nM). FERb 033 shows 62-fold selectivity over ERα.

Isopaucifloral F ((±)-Isopaucifloral F) is a Resveratrol (HY-16561)-derived sesquiterpenes. Isopaucifloral F is an orally active ERβ agonist (EC₅₀: 46.96 μM). Isopaucifloral F has antiosteoporosis activity. LD₅₀ in rats: > 5 mg/kg.

rel-Erteberel is rel isomer of Erteberel (HY-18295). Erteberel is a potent and selective estrogen receptor beta (ERβ) agonist with K_i and EC₅₀ of 1.54 nM and 3.61 nM, respectively. Erteberel has anti-tumor activities.

ERβ agonist-1 (Compound 8) is a dual-active selective ERβ agonist (EC₅₀: 46.8 nM) and AR antagonist (IC₅₀: 1555 nM). ERβ agonist-1 activates ERβ signaling by binding to ERβ and inhibits AR activity. ERβ agonist-1 retains selective ERβ agonist activity in mouse models and can be used to study prostate cancer.

EGX358 is a selective, orally active estrogen receptor β (ERβ) agonist with an EC₅₀ of 27.4 nM for ERβ. EGX358 enhances object recognition ability, spatial memory and memory consolidation, and attenuates drug-induced vasomotor responses. EGX358 alleviates partial uterine atrophy without inducing uterine hypertrophy, while it does not alter anxiety-like behavior, depression-like behavior or body weight. EGX358 can be used in research related to Alzheimer's disease and menopause.

Estrogen receptor modulator 6 (compound 3a) is a selective estrogen receptor (ER) β agonist (K_i=0.44 nM). Estrogen receptor modulator 6 displays 19-fold selectivity for ERβ over ERα(K_i=8.4 nM).