ERα Agonist

Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).

SERT-IN-4 is a brain-penetrant and orally active SERT inhibitor and ERβ agonist with human SERT IC₅₀ of 16.92 nM and human ERβ EC₅₀ of 3.66 nM. SERT-IN-4 inhibits SERT-mediated substrate transport, increases hippocampal serotonin levels, modulates p-CREB and BDNF expression.SERT-IN-4 reduces immobility in CUMS mice, improves social interaction and reduces inactivity in CSDS mice.SERT-IN-4 can be used for the research of major depressive disorder.

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.

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.

(-)-(E)-Guggulsterone ((E)-Guggulsterone) is an orally active natural stereoisomer of Guggulsterone (HY-107738). (-)-(E)-Guggulsterone is an antagonist for the Farnesoid X Receptor (FXR) with an IC₅₀ of 24.06 μM and possesses potent hypolipidemic properties. (-)-(E)-Guggulsterone suppresses dengue virus (DENV) replication by upregulating antiviral interferon responses by inducing HO-1 expression via Nrf2 activation. (-)-(E)-Guggulsterone exhibits antibacterial activities against Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa. (-)-(E)-Guggulsterone has cardiac protective and antioxidant activities in rats.

Estrogen receptor-agonist-1 (compound 4e) is a estrogen receptor (ER) agonist that binds to ERα with high affinity.

GTX-758 is an orally active, nonsteroidal, selective agonist of ERα. GTX-758 plays an important role in castration resistant prostate cancer (CRPC) research.

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.

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.

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).