Estrogen receptor 选择性抑制剂 | 激活剂 | 激动剂 | 拮抗剂 | 化学产品 | 调节剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S8372 AZD9496

AZD9496是口服的雌激素受体抑制剂,在临床肿瘤模型中,能阻止ER阳性以及携带ESR1突变的乳腺肿瘤的生长。

Selective
S3929 Liquiritigenin

Liquiritigenin (4',7-Dihydroxyflavanone), the most active estrogenic compound from the root of Glycyrrhizae uralensis Fisch, selectively binds to ERβ with an IC50 value of 7.5 μM and activates multiple ER regulatory elements and native target genes with Erβ but not ERα.

Selective
S8686 PHTPP

PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.

Selective
S4629 Chlorotrianisene

Chlorotrianisene是一种合成的、非类固醇的雌激素。是选择性的雌激素受体调节剂。

Selective
S2473 Hexestrol

Hexestrol与ERαERβ结合,EC50分别为0.07 nM和0.175 nM。

Selective ERβ, EC50: 0.175 nM; ERα, EC50: 0.07 nM
S9609 Amcenestrant (SAR439859)

SAR439859 is an orally available, selective and nonsteroidal estrogen receptor degrader (SERD) with potential antineoplastic activity.

Selective ERα, EC50: 0.2 nM
S8746 H3B-5942

H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both ERα WT and ERα mutation. The Ki values are 1 nM and 0.41 nM, respectively.

Selective ERα (Y537S), Ki: 0.41 nM; ERα WT, Ki: 1 nM
S1191 Fulvestrant (ICI-182780)

Fulvestrant是一种Estrogen receptor(ER)拮抗剂, 无细胞试验中IC50为0.094 nM。

Selective ER, IC50: 0.94 nM
S9520 Lasofoxifene Tartrate

Lasofoxifene Tartrate is a third-generation, non-steroidal selective estrogen receptor modulator (SERM) which binds with high affinity to the human estrogen receptor-α with IC50 value of 1.5 nM.

Selective estrogen receptor, IC50: 1.5 nM
S4110 Estradiol Benzoate

Estradiol Benzoate是一种雌激素类似物,可以与人源,鼠源以及鸡的ERα结合,IC50范围22-28 nM。

Selective mERα, IC50: 2.3 nM; hERα, IC50: 28 nM
S1227 Raloxifene HCl

Raloxifene HCl是estrogen(雌性激素)拮抗剂,抑制人体胞浆醛氧化酶催化的酞嗪氧化活性,IC50为5.7 nM。

Selective ER, IC50: 5.7 nM
S5781 Raloxifene

Raloxifene (Keoxifene, Pharoxifene, LY-139481, LY-156758, CCRIS-7129) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women.

Selective ER, IC50: 5.7 nM
S7855 Brilanestrant (GDC-0810)

Brilanestrant (GDC-0810, ARN-810) is a potent ER-α binder (ER-α, IC50 = 6.1 nM; ER-β, IC50 = 8.8 nM), a full transcriptional antagonist with no agonism and displays good potency and efficacy in ER-α degradation (EC50 = 0.7 nM) and MCF-7 breast cancer cell viability (IC50 = 2.5 nM) assays with good selectivity over other nuclear hormone receptors.

Selective ERβ, IC50: 8.8 nM; ERα, IC50: 6.1 nM
S0851 G-1

G-1 is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM.

Selective GPR30, Ki: 11 nM
S2128 Bazedoxifene (WAY-140424) HCl

Bazedoxifene HCl是一种新型非甾类基于吲哚的雌激素受体调节剂(SERM),靶点有ERαERβIC50分别为23nM和89nM。

Selective ERβ, IC50: 89 nM; ERα, IC50: 23 nM
S9629 Elacestrant (RAD1901) Dihydrochloride

Elacestrant is an orally available selective estrogen receptor degrader (SERD) with IC50 of 48 nM and 870 nM for ERα and ERβ, respectively.

Selective ERα, IC50: 48 nM; ERβ, IC50: 870 nM
S5676 Zearalenone

Zearalenone (F2 toxin, RAL) is a non-steroidal estrogenic mycotoxin that acts by binding the estrogen receptor (ER).

Selective ERα, IC50: 240.4 nM; ERβ, IC50: 165.7 nM
S5464 Psoralidin

Psoralidin, a naturally occurring coumestan isolated from the fractions of organic solvents such as ethylacetate, hexane, or n-butanol of the seed extract of Psoralea corylifolia L., has a variety of biological activities such as anticancer, antioxidant, antibacterial, antidepressant, anti-inflammatory activities, and regulation of insulin signaling. It is an agonist for both estrogen receptor (ER)α and ERβ with binding affinities (IC50s) of 1.03 and 24.6 μM, respectively.

Selective ERβ, IC50: 24.6 μM; ERα, IC50: 1.03 μM
S4046 Estradiol Cypionate

Estradiol Cypionate是雌二醇的17 β-环戊基丙酸酯,可以通过雌激素受体抑制ET-1的合成。

Selective
S7839 Endoxifen HCl

Endoxifen HCl,Tamoxifen的活性代谢产物,是一种有效的选择性estrogen receptor拮抗剂。Phase 2。

Selective
S1972 Tamoxifen (ICI 46474) Citrate

Tamoxifen Citrate是一种雌激素受体拮抗剂,通过竞争性抑制雌激素结合发挥作用。

Selective
S2561 Clomifene citrate

Clomifene citrate 是一种选择性雌激素受体调节剂,用于诱导排卵。

Selective
S4285 Ospemifene

Ospemifene 是一种非激素的selective estrogen receptor modulator (SERM), 用于性交疼痛治疗。

Selective
S1625 Ethinyl Estradiol

Ethinyl Estradiol 是一种口服生物有效的雌激素,在几乎所有的现代复方口服避孕药丸的配方中使用。

Selective
S1238 Tamoxifen (ICI 46474)

Tamoxifen作用于乳腺组织,是一种雌激素受体拮抗剂。

Selective
S3149 Estradiol valerate

Estradiol valerate是一种人工合成的酯,用于治疗更年期症状及激素不足。

Selective
S4418 Phenol Red sodium salt

Phenol Red sodium salt (Phenolsulfonephthalein sodium salt) is used ubiquitously as a pH indicator in tissue culture media ranging from 6.8 (yellow) to 8.2 (red). Phenol red binds to the estrogen receptor of MCF-7 human breast cancer cells.

Selective
S2125 Mestranol

Mestranol是炔雌醇3-甲基醚,是一种高效的estrogen receptor 激动剂同时也是第一个用于口服的避孕药。

Selective
S2450 Equol

Equol是是大豆的代谢物,是人类的一种重要的异黄酮,与5α-DHT特异性结合,对重组雌激素受体ERβ具有适度的亲和力。Phase 2。

Selective
S6651 G15 (GRB-G15)

G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM.

Selective
S1665 Estrone

Estrone是一种雌激素。

Selective
S1776 Toremifene Citrate (NK 622)

Toremifene Citrate是一种可口服的选择性的雌激素受体调节剂(SERM),用于乳腺癌的治疗。

Selective
S1859 Diethylstilbestrol

Diethylstilbestrol是一种人工合成的非甾体类雌激素,用于治疗绝经期和绝经后的疾病。

Selective
S8958 AZD9833

AZD9833 is an orally available and selective estrogen receptor degrader (SERD) with antineoplastic activity.

Selective
S2167 Bazedoxifene (TSE-424) acetate

Bazedoxifene Acetate是第三代选择性雌激素受体调节剂(SERM)。

Selective
S4440 2-Phenylacetamide

2-Phenylacetamide, the main compound isolated from the seeds of Lepidium apetalum Willd (LA) with estrogenic activities, increases the expression of Estrogen receptorα (ERα), ERβ and GPR30 in the uterus and MCF-7 cells.

Selective
S2466 Estriol

Estriol作用于雌激素受体阴性乳腺癌细胞,拮抗G-蛋白偶联雌激素受体。

Selective
S5393 Cyclofenil

Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than Erα.

Selective
S1709 Estradiol

Estradiol是一种主要的性激素。

Selective
S0503 Estrogen receptor modulator 1

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

Selective ER, pIC50: 0.46