estrogen receptor modulator

Estrogen receptor modulator 1 causes regression of Tamoxifen-resistant, hormone-independent xenograft tumors. Estrogen receptor modulator 1 is an orally active and selective estrogen receptor modulator (SERM) (pIC50: 0.46).

Estrogen Receptor Modulator 8 (compound 4) is an orally active inhibitor targeting Estrogen Receptor/ERR α with potent efficacy (IC50 = 0.437 nM in MCF-7 cells) and effectively hampers MCF-7 cell proliferation (IC50 = 0.1 nM) [1].

Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). It has the capability to induce apoptosis and block cells at the G1/G0 phase, making it applicable in cancer research [1].

Estrogen receptor modulator 6 (compound 3a) is a highly specific and potent agonist of the estrogen receptor (ER) β, exhibiting remarkable affinity (K i = 0.44 nM) and impressive 19-fold selectivity for ERβ over ERα, as evidenced by its affinity (K i = 8.4 nM).

Estrogen Receptor Modulator 7 is a potent modulator of estrogen receptors, utilized in cancer research [1].

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.

AMPA receptor modulator-1 can be activated by glutamate, thereby modulating ion channels.

AMPA receptor modulator-2 (Example 134) is an AMPA receptor modulator with a pIC50 of 10.1 for TARPγ2 dependent AMPA receptor[1]. pIC50 = -lgIC50. [1]. BERRY CYNTHIA G B (US), et al. AZABENZIMIDAZOLES AND THEIR USE AS AMPA RECEPTOR MODULATORS. Patent. WO2016176460.

Glucocorticoid receptor modulator 1 is a potent, orally active, non-steroidal selective glucocorticoid receptor modulator, exhibiting IC50 values of 9 nM and 130 nM against NF-κB and AP-1, respectively. It effectively reduces the expression of inflammatory factors such as IL-6, IL-1β, and TNF-α, and alleviates dermatitis in mice.

NMDA receptor regulator 6 (Compound 183) is an effective NMDA receptor regulator and has research value in neurological disorders.

Estrogen Receptor Antagonist 4 is a potent inhibitor of the estrogen receptor (ER), crucial for regulating cell growth, differentiation, and apoptosis. This compound holds promise for cancer research[1].

NOT Receptor Modulator 1 (2-(3-(2-(4-chlorophenyl)imidazo[1,2-a]pyridin-6-yl)phenyl)propan-2-ol) is a modulator of nuclear receptor NOT.

NMDA receptor modulator 3 (Compound 99) is a potent NMDA receptor modulator useful in neurological disorder research [1].

Estrogen receptor antagonist 3 is a potent degradation agent of the estrogen receptor (ER). Estrogen signaling systems regulate cell growth, differentiation, and apoptosis, and estrogen receptor antagonist 4 has shown potential for cancer research.

Toll-like receptor modulator is a TLR7 8 modulator that regulates immune function.

Estrogen receptor antagonist 5 is a potent inhibitor of the Estrogen receptor, a ligand-activated transcriptional regulatory protein that interacts with endogenous estrogens and mediates various biological effects. [Estrogen receptor antagonist 5] shows promise for studies on metastatic disease.

Estrogen Receptor Antagonist 7 (Compound 13) is a potent antagonist of estrogen receptors (ER), demonstrating antiproliferative effects against breast and ovarian cancer cells, along with anticancer and anti-uterotrophic activities [1].

Opioid receptor modulator 1 is a modulator of the opioid receptor.

Estrogen receptor antagonist 2 is a selective down-regulator of the estrogen receptor, with research potential for breast cancer disease. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development.

GPR52 receptor modulator 1, a compound delineated as per Procedure 1, is a modulator of the GPR52 receptor, offering research potential in the investigation of neuropsychiatric diseases [1].

AMPA Receptor Modulator-5 (Example 217) serves as an AMPA receptor modulator, utilized in neurological disease research [1].

Estrogen receptor α antagonist 1 (compound 35) is a highly selective antagonist of estrogen receptor α, demonstrating an IC50 of 0.02 μM against this receptor and also affecting estrogen receptor β. This compound is utilized in tumor research.

Estrogen receptor antagonist 1 is a potent inhibitor of the estrogen receptor, demonstrating research potential in breast cancer disease.

σ 1 Receptor/ μ Opioid receiver modulator 1 (Compound 44) is an effective σ 1 receptor antagonist (Ki=1.86 nM) and μ Opioid receptor agonists (Ki=2.1 nM). Opioid receptor modulator 1 shows potent analgesic activity, and can be used for the research of neuropathic pain.

NMDA receptor modulator 2 (Compound 1) is a potent NMDA receptor modulator suitable for neurological disorder research [1].

Orexin Receptor Modulator-1 is a compound utilized in the study of various conditions including substance addiction, panic disorder, anxiety, post-traumatic stress disorder (PTSD), pain, depression, seasonal affective disorder (SAD), eating disorders, and hypertension [1].

AMPA Receptor Modulator-4, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD), serves as an orally active positive allosteric modulator of the AMPA receptors (AMPAR PAMs). This compound is capable of crossing the blood-brain barrier and has been found to enhance cognitive performance and working memory in mice [1].

Estrogen receptor-IN-1 (compound 16) is an effective estrogen receptor (ER) inhibitor with IC50 values of 13 μM for ERα and 5 μM for ERβ, respectively [1].

NMDA receptor modulator 5 (Compound 195), a potent NMDA receptor modulator, shows promise for neurological disorder research [1].

GluN2B receptor modulator-1 is a potent and selective allosteric modulator of the GluN2B receptor, demonstrating negative modulation by inhibiting receptor activity and exhibiting high selectivity towards the GluN2B subunit, with an IC50 value of 31 nM.

NMDA receptor modulator 4 (Compound 169) is a potent NMDA receptor modulator used for neurological disorder research [1].

AMPA receptor modulator-6, an AMPA receptor positive allosteric modulator (PAM), is utilized in the research of neurological diseases [1].

Estrogen receptor β antagonist 2 is a selective and potent estrogen receptor β (ERβ) antagonist, with an IC50 of 109.10 μM for ERα and 0.63 μM for ERβ.

GABAA receptor modulator-2 (Compound 20) is a selective, orally active α5-GABAAR negative conformation modulator (Ki: 4.1 nM) that exhibits high metabolic stability and a good central nervous system safety profile.

Estrogen receptor antagonist 6, also known as Compound 166, is a potent antagonist of the ligand-activated transcriptional regulatory protein Estrogen receptor, which interacts with endogenous estrogens to mediate various biological effects.

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.

Raloxifene hydrochloride (LY156758 hydrochloride) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.

Clomiphene citrate (NSC 35770) is a selective estrogen receptor modulator.

Ospemifene (FC-1271a) is a new selective non-hormonal estrogen receptor modulator (SERM) that is used for the treatment of moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause. FDA approved on February 26, 2013.

Bazedoxifene acetate (WAY-TES 424) is a novel selective estrogen receptor modulator (SERM).

Tamoxifen is an antineoplastic nonsteroidal selective estrogen receptor modulator (SERM).

SNG-1153 is a estrogen receptor ER-alpha36 modulator.

Fispemifene (HM-101) is an estrogen receptor modulator (SERM) used to treat genitourinary syndromes and vaginal atrophy.

Pipendoxifene hydrochloride is a selective modulator of estrogen receptor.

CHF-4227 is a novel, potent and selective estrogen receptor modulator that reduces cholesterol and LDL cholesterol concentrations.

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.

(E Z)-4-Hydroxytamoxifen (Afimoxifene), the active metabolite of tamoxifen, is a selective estrogen receptor (ER) modulator widely used in the therapeutic and chemopreventive treatment of breast cancer.

Calycosin (Cyclosin) acts as a selective estrogen receptor modulator. Calycosin induces apoptosis in human ovarian cancer SKOV3 cells by activating caspases and Bcl-2 family proteins. Calycosin suppresses breast cancer cell growth via ERβ-dependent regulation of IGF-1R, p38 MAPK and PI3K/Akt pathways. Calycosin has antineoplastic effects against osteosarcoma through inducing apoptosis showing in vitro and in vivo investigations. Calycosin was shown to induce angiogenesis in human umbilical vein endothelial cell cultures (HUVEC) in vitro. Calycosin may be an effective skin-lightening agent that regulates the expression of melanogenic enzymes. Calycosin exhibited tyrosinase inhibitory activity with an IC(50) value of 38.4 microM.

Toremifene (GTx 006) is a selective estrogen-receptor modulator (SERM).

Lasofoxifene Tartrate (CP-336156) is a third-generation, non-steroidal selective estrogen receptor modulator.