GPR30 agonist-1 is a G protein-coupled receptor 30 (GPR30) agonist. GPR30 agonist-1 exerts vasorelaxant effects[1].
DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an >IC50 value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM)[1].
Raloxifene 4-Monomethyl Ether (Compound 37) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 1 μM and a pIC50 of 6[1].
Isocurcumenol, an estrogen receptor alpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1µg/mL and 178.2 µg/mL in DLA and KB cells, respectively[1][2].
SLU-PP-915 is an agonist of ERR. SLU-PP-915 has an EC50 value of approximately 400 nM for ERRα, ERRβ, and ERRγ. SLU-PP-915 has potential application in maintaining oxidative metabolism and heart failure[1][2][3].
Cholesterol-d1 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins[1][2]. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist[3][4].
Arzoxifene hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.
Estrogen receptor β antagonist 2 is a potent and selective estrogen receptor β (ERβ) antagonist with IC50s of 109.10, 0.63 µM for Erα and Erβ, respectively[1].
N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation[1][2][3].
Cholesterol-d6 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins[1][2]. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist[3][4].
Fulvestrant is a potent Estrogen Receptor antagonist with an IC50 of 9.4 nM.
Estropipate is a form of estrogen, used to treat symptoms of menopause, also used to prevent osteoporosis.
Taragarestrant (D-0502) meglumine is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant meglumine shows potent activity in various ER+ breast cancer cell lines and xenograft models[1][2].
Levormeloxifene (fumarate) is a stable salt form of Levormeloxifene. Levormeloxifene (fumarate) is an estrogen receptor modulator that plays an important role in prevention of postmenopausal bone loss[1].
WAY-169916 is a pathway-selective ligand of ER (estrogen receptor) that acts by inhibiting NF-kB transcriptional activity. WAY-169916 has potent anti-inflammatory effect[1].
Estradiol dipropionate is a combined estrogen-progesterone, acts as an estrogen and progesterone agonist[1].
Zuclomiphene-d5 (citrate) is the deuterium labeled Zuclomiphene citrate[1]. Zuclomiphene citrate is a cis isomer of Clomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent[2][3][4][5].
Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile[1].
ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader 5 can be used for the research of breast cancer[1].
Elacestrant (RAD1901) is a selective and orally available estrogen receptor (ER) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. [1][2]. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[3].
Yp537 is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor[1].
Gypenoside XVII, a novel phytoestrogen belonging to the gypenosides, can activate estrogen receptors.
H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA).
Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.
Estradiol benzoate-d3 is the deuterium labeled Estradiol benzoate. Estradiol Benzoate (β-Estradiol 3-benzoate), a prodrug of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability[1][2][3][4].
Liquiritigenin, a flavanone isolated from Glycyrrhiza uralensis, is a highly selective estrogen receptor β (ERβ) agonist with an EC50 of 36.5 nM for activation of the ERE tk-Luc.
Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) inhibitor with Ki and EC50 of 1.54 nM and 3.61 nM, respectively[1]. Anti-tumor activities[2].
Propyl pyrazole triol (PPT) is an estrogen receptor alpha (ERσ) 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%)[1].
Toremifene-d6 (Z-Toremifene-d6) citrate is the deuterium labeled Toremifene citrate. Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively[1][2].