erβ

Erteberel (LY500307) is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.

Serba-2 is an agonist of benzopyran selective estrogen receptor beta.

Prinaberel (ERB 041) is a selective and potent estrogen receptor β (ERβ) agonist with anticancer activity that restores or increases ERβ expression and reduces cancer cell proliferation in mouse squamous cell carcinoma and human carcinoma cells. Prinaberel exhibits anti-inflammatory activity, inhibits the NFκB pro-inflammatory signaling pathway, and induces apoptosis of ovarian cancer cells. study endometriosis.

Liquiritigenin (4',7-Dihydroxyflavanone), a flavonoid aglycone from licorice, is a highly selective estrogen receptor β (ERβ) agonist.

Alpha-Estradiol (Epiestradiol) is an estrogen that inhibits 5alpha-reductase and has potential in the study of androgenetic alopecia.

NXT629 is a selective and highly efficient PPAR-α antagonist with anticancer activity. It inhibits PPARδ, PPARγ, Erβ, GR, and TRβ and can be used in research on ovarian cancer and melanoma.

Elacestrant (RAD1901) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.Elacestrant  is an orally available selective estrogen receptor degrader .

(+)-Medicarpin, a pterocarpan, is an isoflavonoid compound derived from medicinal plant species such as Sophora japonica, Zollernia paraensis, Platymiscium yucatamun, Machaerium aristulatum, and Platymiscium floribundum. It potently inhibits osteoclastogenesis and facilitates bone healing and increased bone mass through osteoblast differentiation, mediated by the estrogen receptor (ER) β.

ERα ERβ antagonist-1 (Compound 10) functions as a partial antagonist of both ERα and ERβ. It reduces the activity of ERα and ERβ in HepG2 liver cells in a dose-dependent manner.

ERβagonist-1 (Compound 8) functions as a dual-active selective ERβ agonist (EC50: 46.8 nM) and an AR antagonist (IC50: 1555 nM). By binding to ERβ, it activates its signaling pathways while simultaneously inhibiting AR activity. Retaining selective ERβ agonist activity in mouse models, ERβagonist-1 is applicable in prostate cancer research.

Bavachin (Corylifolin) is a phytoestrogen that activates the estrogen receptors ERα and ERβ.

(±)-Equol ((R,S)-Equol) is a non-steroidal estrogen produced from the metabolism of the isoflavonoid phytoestrogen daidzen by human intestinal microflora. The estrogen receptor (ER) agonist activity of the naturally occurring (S)-enantiomer (EC50 = 85 and 65 nM for human ERα and ERβ, respectively) is similar to that of genistein but exceeds that of daidzein. (±)-Equol preferentially binds ERβ (Ki = 0.73 nM) and demonstrates approximately 9-fold lower affinity for ERα (Ki = 6.41 nM). (±)-Equol is also a potent antagonist of dihydrotestosterone, which has important implications for prostate cancer and other androgen-mediated pathologies.

PHTPP is a selective ERβ antagonist.

Bazedoxifene hydrochloride (TSE 424 hydrochloride) is an orally active, selective, and potent estrogen receptor modulator (SERM) that crosses the blood-brain barrier and is an inhibitor of IL-6/GP130 protein interactions with high affinity for ERα and ERβ. It has a high affinity for ERα and ERβ and can be used to study postmenopausal osteoporosis and vasodilator-related diseases.

Hexestrol (Hexanoestrol) binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively.

Fulvestrant (ZM 182780) is an estrogen receptor (ER) antagonist (IC50=9.4 nM) and an agonist of GPR30. Fulvestrant has antitumor activity, inhibiting cell proliferation and inducing apoptosis and autophagy.

4-Hydroxytamoxifen (ICI 79280) is the active metabolite of Tamoxifen, an estrogen receptor modulator (SERM) with selective and oral potency. 4-Hydroxytamoxifen has antitumor activity and may be used in breast cancer research.

Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

Zindoxifene (D 16726) is an anti-estrogenic compound with antitumor activity that can be used in studies of breast and prostate cancer.

Estrogen receptor antagonist 8 acts as an estrogen receptor (ER) antagonist with anti-uterine activity and potential anti-tumorigenic activity and can be used to study ovarian dysfunction.

Estradiol (E2) is a naturally occurring steroidal sex hormone that is essential for female fertility and maintenance of secondary sexual characteristics. Estradiol upregulates IL-6 expression through estrogen receptor beta (ERβ).

Fluticasone propionate (CCI-187881), derived from fluticasone used to remedy asthma and allergic rhinitis, is a high affinity, selective GR (glucocorticoid receptor) agonist.

Ethisterone (17α-Ethynyltestosterone) is a progestogen hormone.

Progesterone is a steroid hormone that regulates the menstrual cycle and is essential for pregnancy. It is also commonly used to induce melasma models.