Estrogen Receptor/ERR Ligand

ERα ligand 4 is a ligand of ERα and can be used for the synthesis of PROTACs, such as NEP168 (HY-180959).

Ent-Estradiol is the enantiomer of Estradiol (HY-B0141). Ent-Estradiol is a highly selective estrogen receptor ligand, but does not possess estrogenic activity. Ent-Estradiol displays IC₅₀ values of 24.9 nM, 9.59 nM and 8.17 nM for human, rat and mouse ERβ, and 151 nM, 246 nM and 268 nM for human, rat and mouse ERα, respectively. Ent-Estradiol can be used for the study of menopausal physiological changes.

ERα ligand 5 (Compound 53) is a ERα ligand that can be used for the synthesis of PROTACs, such as ERD-308 (HY-128600).

HDAC6/ERα ligand-1 is a dual-target ligand with inhibitory activity against both estrogen receptor α (ERα) and histone deacetylase 6 (HDAC6). HDAC6/ERα ligand-1 can be used to synthesize PROTACs, such as PROTAC HDAC6/ERα degrader 1 (HY-187387). HDAC6/ERα ligand-1 binds to the ligand-binding pocket of ERα and forms hydrogen bonds with specific residues in helices 10, 11 and 12. HDAC6/ERα ligand-1 binds stably to HDAC6 and forms hydrogen bonds with specific residues of this protein. HDAC6/ERα ligand-1 can be used in breast cancer research.

ER ligand-3 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). ER ligand-3 can be used for the synthesis of PROTAC ER Degrader-12 (HY-160264).

Fluoroestradiol is an Estrogen receptor PET imaging tracer precursor. Fluoroestradiol, when radiolabeled with ¹⁸F, can be used as an Estrogen receptor PET imaging tracer. ¹⁸F-Fluoroestradiol exhibits the highest uptake selectivity and target-to-background ratio among
several 18F-labeled estrogens. ¹⁸F-Fluoroestradiol has demonstrated Estrogen receptor expression in normal brain tissues and in meningiomas. ¹⁸F-Fluoroestradiol can quantify regional Estrogen receptor expression in breast cancer. ¹⁸F-Fluoroestradiol has potential applications in assessing and monitoring heterogeneity in ovarian cancer.

4,4'-(Cyclohexylidenemethylene)diphenol (Compound 2) is a symmetric cyclic nonsteroidal estrogen. 4,4'-(Cyclohexylidenemethylene)diphenol has high binding affinity for estrogen receptors ERα and ERβ.

ER ligand-10 (Compound 11a) is a weak ERa and ERβ ligand, and shows weak estrogenic activity.

Metahexestrol is an estrogen receptor (E2R) inhibitor with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cells (ED₅₀ = 1.0 μM). Additionally, Metahexestrol also exhibits inhibitory effects in estrogen receptor-negative MDA-MB-231 cells, and its antiproliferative activity cannot be reversed by estrogen, suggesting that its mechanism of action may be partially independent of the E2R pathway. Metahexestrol can be used in research on estrogen-dependent breast cancer.

Epimedin B (Standard) (Epmedin B (Standard)) is the analytical standard of Epimedin B (HY-N0259). This product is intended for research and analytical applications. Epimedin B (Epmedin B) is a flavonoid active component found in Epimedium, with oral activity, and exhibits anti-osteoporotic and neuroprotective effects. Epimedin B inhibits RANKL-induced osteoclast differentiation, F-actin ring formation, and mature osteoclast bone resorption, inhibits the phosphorylation of JNK, p38 MAPK, PI3K, and AKT, activates the AMPK-Nrf2 antioxidant pathway, and reduces cellular and mitochondrial ROS. Epimedin B acts on ESR1 and exerts its effects via GPER. Epimedin B alleviates bone loss and improves bone microstructure in vivo, and in Parkinson's models protects dopaminergic neurons and maintains striatal dopamine levels through anti-apoptotic and anti-endoplasmic reticulum stress effects. Epimedin B can be used for research related to osteoporosis, diabetic osteoporosis, and Parkinson's disease.

Amsonic acid is an orally active weak estrogen receptor ligand with uterotrophic activity. In the weanling female rat model, Amsonic acid exhibits a uterotrophic effect consistent with that of diethylstilbestrol at equiactive doses. Amsonic acid can also be used in studies related to erectile dysfunction.

D 15414 is an estrogen receptor ligand and the hydroxylated metabolite of Zindoxifene (HY-106056). D 15414 binds to estrogen receptors and mediates estrogen-like cellular responses. D 15414 stimulates prolactin production, progesterone receptor synthesis and cancer cell proliferation. D 15414 inhibits the growth of hormone-dependent human breast cancer cells. D 15414 can be used in research related to breast cancer and hormone-dependent human breast cancer.

Diisopropyl phthalate (Standard) (DiPP (Standard)) is the analytical standard of Diisopropyl phthalate (HY-W011926). This product is intended for research and analytical applications. Diisopropyl phthalate (DiPP) is a phthalate diester, which is widely used as an additive in plastics and consumer products. Diisopropyl phthalate has a weak binding ability to the recombinant human estrogen receptor, with an IC₅₀ of 41000 μM.