エストロゲン/プロゲストゲン受容体

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1304 Megestrol Acetate <1 mg/mL 33 mg/mL '15 mg/mL
S8372 AZD9496 <1 mg/mL 88 mg/mL 88 mg/mL
S9506 Danazol -1 mg/mL 67 mg/mL -1 mg/mL
S4440 2-Phenylacetamide 27 mg/mL 27 mg/mL ''27 mg/mL
S9207 Gypenoside XVII -1 mg/mL 100 mg/mL -1 mg/mL
S5364 DY131 <1 mg/mL 62 mg/mL <1 mg/mL
S1191 Fulvestrant <1 mg/mL 100 mg/mL '100 mg/mL
S2606 Mifepristone <1 mg/mL 85 mg/mL '19 mg/mL
S9609 SAR439859 <1 mg/mL 100 mg/mL '''100 mg/mL
S0851 G-1 <1 mg/mL 82 mg/mL '''<1 mg/mL
S8958 AZD9833 <1 mg/mL 95 mg/mL ''''95 mg/mL
S2466 Estriol <1 mg/mL 57 mg/mL 10 mg/mL
S6651 G15 (GRB-G15) <1 mg/mL 74 mg/mL ''<1 mg/mL
S8746 H3B-5942 <1 mg/mL 99 mg/mL 13 mg/mL
S8686 PHTPP <1 mg/mL 50 mg/mL 84 mg/mL
S7855 Brilanestrant (GDC-0810) <1 mg/mL 89 mg/mL 89 mg/mL
S7839 Endoxifen HCl <1 mg/mL 74 mg/mL 74 mg/mL
S1709 Estradiol <1 mg/mL 54 mg/mL '5 mg/mL
S3449 GSK5182 <1 mg/mL 84 mg/mL '''84 mg/mL
S4097 Dydrogesterone <1 mg/mL 63 mg/mL '63 mg/mL
S2604 Dehydroepiandrosterone (DHEA) <1 mg/mL 57 mg/mL '57 mg/mL
S2450 Equol <1 mg/mL 48 mg/mL 48 mg/mL
S1727 Levonorgestrel <1 mg/mL 45 mg/mL '2 mg/mL
S2567 Medroxyprogesterone acetate <1 mg/mL 12 mg/mL ''12 mg/mL
S2473 Hexestrol <1 mg/mL 42 mg/mL 42 mg/mL
S1705 Progesterone <1 mg/mL 22 mg/mL '63 mg/mL
S1859 Diethylstilbestrol <1 mg/mL 54 mg/mL 54 mg/mL
S1625 Ethinyl Estradiol <1 mg/mL 59 mg/mL 59 mg/mL
S3149 Estradiol valerate <1 mg/mL 71 mg/mL <1 mg/mL
S2125 Mestranol <1 mg/mL 15 mg/mL 25 mg/mL
S4110 Estradiol Benzoate <1 mg/mL 75 mg/mL <1 mg/mL
S3167 Altrenogest <1 mg/mL 62 mg/mL 2 mg/mL
S5872 Estradiol dipropionate <1 mg/mL 21 mg/mL 20 mg/mL
S3617 (20S)-Protopanaxatriol <1 mg/mL 95 mg/mL ''95 mg/mL
S6601 (±)-Equol <1 mg/mL 48 mg/mL 48 mg/mL
S5676 Zearalenone <1 mg/mL 64 mg/mL 64 mg/mL
S4154 Cholesterol <1 mg/mL 0.03 mg/mL <1 mg/mL
S5288 Estropipate -1 mg/mL 87 mg/mL -1 mg/mL
S4046 Estradiol Cypionate <1 mg/mL 79 mg/mL 55 mg/mL
S4638 Desogestrel <1 mg/mL 62 mg/mL 62 mg/mL
S3657 Promestriene 3 mg/mL 65 mg/mL 65 mg/mL
S3929 Liquiritigenin -1 mg/mL 51 mg/mL -1 mg/mL
S1858 Dienestrol -1 mg/mL 53 mg/mL -1 mg/mL
S4883 Lynestrenol -1 mg/mL 56 mg/mL -1 mg/mL
S3635 Medroxyprogesterone <1 mg/mL 68 mg/mL 14 mg/mL
S4674 Hydroxyprogesterone caproate <1 mg/mL 85 mg/mL '85 mg/mL
S3671 Quinestrol <1 mg/mL 72 mg/mL 72 mg/mL
S0407 XCT790 <1 mg/mL 8 mg/mL <1 mg/mL
S4507 17-Hydroxyprogesterone <1 mg/mL 66 mg/mL 66 mg/mL
S4673 Etonogestrel <1 mg/mL 64 mg/mL 64 mg/mL
S7828 Licochalcone A <1 mg/mL 67 mg/mL 67 mg/mL
S5464 Psoralidin <1 mg/mL 67 mg/mL 1 mg/mL
S3160 Ethynodiol diacetate 77 mg/mL 77 mg/mL <1 mg/mL
S2611 Ethisterone <1 mg/mL 0.05 mg/mL <1 mg/mL
S5469 Bavachin <1 mg/mL 64 mg/mL 45 mg/mL
S1972 Tamoxifen Citrate <1 mg/mL 100 mg/mL '''100 mg/mL
S1227 Raloxifene HCl <1 mg/mL 100 mg/mL '<1 mg/mL
S8956 (Z)-4-Hydroxytamoxifen <1 mg/mL 78 mg/mL '''10 mg/mL
S1776 Toremifene Citrate <1 mg/mL 100 mg/mL <1 mg/mL
S2128 Bazedoxifene HCl <1 mg/mL 101 mg/mL '<1 mg/mL
S2561 Clomifene citrate <1 mg/mL 120 mg/mL 11 mg/mL
S3081 Ulipristal acetate <1 mg/mL 83 mg/mL ''14 mg/mL
S1914 Pregnenolone <1 mg/mL 22 mg/mL 22 mg/mL
S2167 Bazedoxifene Acetate <1 mg/mL 100 mg/mL '25 mg/mL
S0503 Estrogen receptor modulator 1 <1 mg/mL 48 mg/mL '36 mg/mL
S9520 Lasofoxifene Tartrate <1 mg/mL 100 mg/mL <1 mg/mL
S4629 Chlorotrianisene <1 mg/mL 76 mg/mL <1 mg/mL
S7827 4-Hydroxytamoxifen (Afimoxifene) <1 mg/mL 77 mg/mL '<1 mg/mL
S2301 Genistin (Genistoside) <1 mg/mL 86 mg/mL 34 mg/mL
S2314 Kaempferol <1 mg/mL 57 mg/mL 3 mg/mL
S5781 Raloxifene <1 mg/mL 95 mg/mL 10 mg/mL
S9122 Tectorigenin -1 mg/mL 60 mg/mL -1 mg/mL
S1238 Tamoxifen <1 mg/mL 74 mg/mL ''74 mg/mL
S4285 Ospemifene <1 mg/mL 75 mg/mL 71 mg/mL
S5393 Cyclofenil -1 mg/mL 21 mg/mL -1 mg/mL
S5219 Allylestrenol <1 mg/mL 60 mg/mL ''60 mg/mL
S4418 Phenol Red sodium salt 15 mg/mL 75 mg/mL ''20 mg/mL
S1251 Dienogest <1 mg/mL 62 mg/mL <1 mg/mL
S1376 Gestodene <1 mg/mL 62 mg/mL 8 mg/mL
S1377 Drospirenone <1 mg/mL 73 mg/mL 11 mg/mL
S1665 Estrone <1 mg/mL 54 mg/mL <1 mg/mL

亜型選択性的な製品

Estrogen/progestogen Receptor製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1304

Megestrol Acetate

Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.

S8372

AZD9496

AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.

S9506

Danazol

Danazol (WIN-17757, 2,3-Isoxazolethisterone) is a synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins.

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.

S9207

Gypenoside XVII

Gypenoside XVII (GP-17, Gynosaponin S), a ginsenoside found in Panax species, has neuroprotective effects and is widely used to prevent cardiovascular disease.

S5364

DY131

DY131 is a potent and selective ERRβ/γ activator. It has no effect on the structurally related receptors ERRalpha or the estrogen receptors alpha and beta (ERalpha/beta).

S1191

Fulvestrant

Fulvestrant (ICI-182780, ZD 9238, ZM 182780) is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.

S2606

Mifepristone

Mifepristone (RU486, C-1073, RU 38486, RU-486, Mifegyne) is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.

S9609

SAR439859

SAR439859 (compound 43d) is an orally available and nonsteroidal selective estrogen receptor degrader (SERD) with potential antineoplastic activity. SAR439859 is a potent estrogen receptor (ER) antagonist with EC50 of 0.2 nM for ERα degradation.

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.

S8958

AZD9833

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

S2466

Estriol

Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.

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.

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.

S8686

PHTPP

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

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.

S7839

Endoxifen HCl

Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.

S1709

Estradiol

Estradiol (17β-estradiol, β-Estradiol, E2, 17β-Oestradiol) is a human sex hormone and steroid, and the primary female sex hormone. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.

S3449

GSK5182

GSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors.

S4097

Dydrogesterone

Dydrogesterone (NSC 92336) is an orally active progestogen which acts directly on the uterus, producing a complete secretory endometrium in an estrogen-primed uterus.

S2604

Dehydroepiandrosterone (DHEA)

Dehydroepiandrosterone (DHEA, Prasterone, Dehydroisoandrosterone) is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.

S2450

Equol

Equol ,a metabolite of soybeans, is an important isoflavone in humans,specifically binds to 5α-DHT, has a modest affinity for recombinant estrogen receptor ERβ. Phase 2.

S1727

Levonorgestrel

Levonorgestrel (D-Norgestrel) is a female hormone that prevents ovulation.

S2567

Medroxyprogesterone acetate

Medroxyprogesterone acetate (MPA, NSC-26386, Medroxyprogesterone 17-acetate, Farlutin) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding.

S2473

Hexestrol

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

S1705

Progesterone

Progesterone (Pregn-4-ene-3,20-dione) is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. A potent agonist of the nuclear progesterone receptor (nPR) with Kd of 1 nM; An agonist of the membrane progesterone receptors(mPRs); An antagonist of the σ1 receptor.

S1859

Diethylstilbestrol

Diethylstilbestrol (Stilbestrol) is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications.

S1625

Ethinyl Estradiol

Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.

S3149

Estradiol valerate

Estradiol is a synthetic ester used to treat menopausal symptoms and hormone deficiencies.

S2125

Mestranol

Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives.

S4110

Estradiol Benzoate

Estradiol benzoate is an estradiol analog which binds to the human, murine and chicken ERα with IC50 of 22-28 nM.

S3167

Altrenogest

Altrenogest (A35957, RU2267) is a progestogen structurally related to veterinary steroid trenbolone.

S5872

Estradiol dipropionate

Estradiol dipropionate (17-Beta-Estradiol-3,17-Dipropionate) is a semisynthetic, steroidal estrogen which has been used in hormone therapy for menopausal symptoms and low estrogen levels in women and in the treatment of gynecological disorders.

S3617

(20S)-Protopanaxatriol

(20S)-Protopanaxatriol (g-PPT, 20(S)-APPT), a neuroprotective metabolite of ginsenoside, protopanaxatriol (g-PPT), is a functional ligand for both GR and ERbeta and could modulate endothelial cell functions through the glucocorticoid receptor (GR) and estrogen receptor (ER).

S6601

(±)-Equol

(±)-Equol, an isoflavandiol estrogen, is a metabolite of the soy isoflavones, daidzin and daidzein.

S5676

Zearalenone

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

S4154

Cholesterol

Cholesterol is the principal sterol of all higher animals required to build and maintain membranes.

S5288

Estropipate

Estropipate (Piperazine estrone sulfate, Estrone sulfate piperazine salt, Pipestrone) is a natural estrogenic substance composed of estrone sulfate and piperazine and is used mainly in menopausal hormone therapy in the treatment of menopausal symptoms.

S4046

Estradiol Cypionate

Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor.

S4638

Desogestrel

Desogestrel (Cerazette, Desogen, Desogestrelum, Org-2969) is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents.

S3657

Promestriene

Promestriene (3-propyl ethyl, 17B-methyl estradiol) is a synthetic estrogen analog that has been reported to significantly improve the symptoms of vaginal atrophy caused by estrogen deprivation in topical application.

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.

S1858

Dienestrol

Dienestrol(Restrol) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist.

S4883

Lynestrenol

Lynestrenol (Ethinylestrenol) is a synthetic progestational hormone, an agonist of the progesterone receptor and has weak androgenic and estrogenic activity.

S3635

Medroxyprogesterone

Medroxyprogesterone (MP) is a synthetic pregnane steroid and a derivative of progesterone. It is a potent progesterone receptor agonist.

S4674

Hydroxyprogesterone caproate

Hydroxyprogesterone Caproate (17α-Hydroxyprogesterone hexanoate, 17α-Hydroxyprogesterone caproate) is a synthetic progestational agent. It binds to and activates nuclear progesterone receptors in the reproductive system and inhibits ovulation and an alteration in the cervical mucus and endometrium.

S3671

Quinestrol

Quinestrol (Ethinylestradiol 3-cyclopentyl ether, EE2CPE, W-3566) is a synthetic, steroidal estrogen which is used in hormone replacement therapy and occasionally to treat breast cancer and prostate cancer.

S0407

XCT790

XCT-790 (Compound 12) is a potent and selective inverse agonist for estrogen-related receptor α (ERRα) with IC50 of 0.37 μM. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ. XCT-790 (Compound 12) significantly inhibits in vivo tumor growth and angiogenesis, and induces apoptosis.

S4507

17-Hydroxyprogesterone

17-Hydroxyprogesterone (17-OHP) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.

S4673

Etonogestrel

Etonogestrel (Implanon, Nexplanon, 3-Oxodesogestrel, 3-keto-Desogestrel) is a synthetic form of the naturally occurring female sex hormone progesterone. It binds to the cytoplasmic progesterone receptors in the reproductive system and subsequently activates progesterone receptor mediated gene expression.

S7828

Licochalcone A

Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.

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.

S3160

Ethynodiol diacetate

Ethynodiol diacetate (8080 CB) is one of the first synthetic progestogens used in contraceptive pills.

S2611

Ethisterone

Ethisterone is a progestogen hormone being considered to treat prostate cancer.

S5469

Bavachin

Bavachin (Corylifolin) is a phytoestrogen purified from natural herbal plants such as Psoralea corylifolia. It acts as a weak phytoestrogen by binding and activating the ER.

S1972

Tamoxifen Citrate

Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.

S1227

Raloxifene HCl

Raloxifene (LY156758, Keoxifene) HCl a selective and orally active estrogen receptor modulator (SERM), which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.

S8956

(Z)-4-Hydroxytamoxifen

(Z)-4-Hydroxytamoxifen ((Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen) is a selective modulator of estrogen receptor (SERM) with IC50 of 3.3 nM for the [3H]oestradiol binding to oestrogen receptor.

S1776

Toremifene Citrate

Toremifene Citrate (NSC 613680) is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer.

S2128

Bazedoxifene HCl

Bazedoxifene HCl is a novel, non-steroidal, indole-based estrogen receptor modulator (SERM) binding to both ERα and ERβ with IC50 of 23 nM and 89 nM, respectively.

S2561

Clomifene citrate

Clomifene Citrate (NSC 35770) is a selective estrogen receptor modulator, used in the treatment of ovulation induction.

S3081

Ulipristal acetate

Ulipristal acetate (CDB-2914) is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.

S1914

Pregnenolone

Pregnenolone is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries.

S2167

Bazedoxifene Acetate

Bazedoxifene Acetate (WAY-140424, TSE-424) is a third generation selective estrogen receptor modulator (SERM).

S0503

Estrogen receptor modulator 1

Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM) with pIC50 of 0.46. Estrogen receptor modulator 1 exhibits potential anti-tumor activity.

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.

S4629

Chlorotrianisene

Chlorotrianisene (tri-p-anisylchloroethylene, TACE, CTA) is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator.

S7827

4-Hydroxytamoxifen (Afimoxifene)

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

S2301

Genistin (Genistoside)

Genistin (Genistoside, Genistine, Genistein 7-glucoside, Genistein glucoside) is an isoflavone found in a number of dietary plants like soy and kudzu. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of Estrogen Receptor α (ERα) signaling pathway.

S2314

Kaempferol

Kaempferol (Robigenin), a natural flavonol, functions as an ERRα and ERRγ inverse agonist. It inhibits topoisomerase I catalyzed DNA religation and may also inhibit the activity of fatty acid synthase.

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.

S9122

Tectorigenin

Tectorigenin (TEC) is an isoflavone isolated from various medicinal plants, such as Pueraria thunbergiana Benth, Belamcanda chinensis, and Iris unguicularis. It has been reported to exert pharmacological actions, including antitumor and antibacterial effects, free radical neutralization, and selective estrogen receptor modulation.

S1238

Tamoxifen

Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis.

S4285

Ospemifene

Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.

S5393

Cyclofenil

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

S5219

Allylestrenol

Allylestrenol is an orally active progestagen of the 19-nortestosterone series resembling progesterone.

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.

S1251

Dienogest

Dienogest (STS 557) is an orally active synthetic progesterone, used for contraception and the treatment of endometriosis.

S1376

Gestodene

Gestodene (SH B 331) is a progestogen hormonal contraceptive.

S1377

Drospirenone

Drospirenone (ZK 3059) is a synthetic progestin that is an analog to spironolactone.

S1665

Estrone

Estrone is an estrogenic hormone.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1304

Megestrol Acetate

Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.

S8372

AZD9496

AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.

S9506

Danazol

Danazol (WIN-17757, 2,3-Isoxazolethisterone) is a synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

S9207

Gypenoside XVII

Gypenoside XVII (GP-17, Gynosaponin S), a ginsenoside found in Panax species, has neuroprotective effects and is widely used to prevent cardiovascular disease.

S5364

DY131

DY131 is a potent and selective ERRβ/γ activator. It has no effect on the structurally related receptors ERRalpha or the estrogen receptors alpha and beta (ERalpha/beta).

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1191

Fulvestrant

Fulvestrant (ICI-182780, ZD 9238, ZM 182780) is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.

2021, 10.1158/1078-0432.CCR-20-2961

2021, 10.1021/acsbiomaterials.0c01803

2021, 23(1):26

S2606

Mifepristone

Mifepristone (RU486, C-1073, RU 38486, RU-486, Mifegyne) is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.

2020, 202021450

2020, 20;6:24

2020, 24;10(1):5363

S9609

SAR439859

SAR439859 (compound 43d) is an orally available and nonsteroidal selective estrogen receptor degrader (SERD) with potential antineoplastic activity. SAR439859 is a potent estrogen receptor (ER) antagonist with EC50 of 0.2 nM for ERα degradation.

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.

S8958

AZD9833

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

S2466

Estriol

Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.

2019, 75(6):1103-1116.e9

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.

2020, 38(1):38-46

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.

S8686

PHTPP

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

2020, 208:111429

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.

2020, 10.1007/s10549-020-05575-9

2019, 51(2):207-216

S7839

Endoxifen HCl

Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.

2021, mjab018

2020, 130:115123

2019, 75(6):1103-1116.e9

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1709

Estradiol

Estradiol (17β-estradiol, β-Estradiol, E2, 17β-Oestradiol) is a human sex hormone and steroid, and the primary female sex hormone. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.

2021, 209:105826

2020, 10(4):1833-1848

2020, 1;248:117449

S3449

GSK5182

GSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors.

S4097

Dydrogesterone

Dydrogesterone (NSC 92336) is an orally active progestogen which acts directly on the uterus, producing a complete secretory endometrium in an estrogen-primed uterus.

S2604

Dehydroepiandrosterone (DHEA)

Dehydroepiandrosterone (DHEA, Prasterone, Dehydroisoandrosterone) is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.

2020, 9e56749

2020, 10.1038/s41416-020-1007-3

, 382(2):195-202

S2450

Equol

Equol ,a metabolite of soybeans, is an important isoflavone in humans,specifically binds to 5α-DHT, has a modest affinity for recombinant estrogen receptor ERβ. Phase 2.

2015, 10.1021/cb5009487

S1727

Levonorgestrel

Levonorgestrel (D-Norgestrel) is a female hormone that prevents ovulation.

2020, 1(2):235-248

S2567

Medroxyprogesterone acetate

Medroxyprogesterone acetate (MPA, NSC-26386, Medroxyprogesterone 17-acetate, Farlutin) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding.

2015, 10.1186/s12990-015-0050-1

S2473

Hexestrol

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

S1705

Progesterone

Progesterone (Pregn-4-ene-3,20-dione) is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. A potent agonist of the nuclear progesterone receptor (nPR) with Kd of 1 nM; An agonist of the membrane progesterone receptors(mPRs); An antagonist of the σ1 receptor.

2020, 10.1111/1759-7714.13528

2019, 75(6):1103-1116.e9

2019, 10:34

S1859

Diethylstilbestrol

Diethylstilbestrol (Stilbestrol) is a synthetic nonsteroidal estrogen, used to prevent miscarriage and other pregnancy complications.

2020, 19;20:58

2020, 10.1007/s13577-020-00425-8

2020, 10.1007/s13577-020-00420-z

S1625

Ethinyl Estradiol

Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.

2020, ddaa244

2020, S0273-2300(20)30246-4

S3149

Estradiol valerate

Estradiol is a synthetic ester used to treat menopausal symptoms and hormone deficiencies.

S2125

Mestranol

Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives.

S4110

Estradiol Benzoate

Estradiol benzoate is an estradiol analog which binds to the human, murine and chicken ERα with IC50 of 22-28 nM.

S3167

Altrenogest

Altrenogest (A35957, RU2267) is a progestogen structurally related to veterinary steroid trenbolone.

S5872

Estradiol dipropionate

Estradiol dipropionate (17-Beta-Estradiol-3,17-Dipropionate) is a semisynthetic, steroidal estrogen which has been used in hormone therapy for menopausal symptoms and low estrogen levels in women and in the treatment of gynecological disorders.

S3617

(20S)-Protopanaxatriol

(20S)-Protopanaxatriol (g-PPT, 20(S)-APPT), a neuroprotective metabolite of ginsenoside, protopanaxatriol (g-PPT), is a functional ligand for both GR and ERbeta and could modulate endothelial cell functions through the glucocorticoid receptor (GR) and estrogen receptor (ER).

S6601

(±)-Equol

(±)-Equol, an isoflavandiol estrogen, is a metabolite of the soy isoflavones, daidzin and daidzein.

S5676

Zearalenone

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

S4154

Cholesterol

Cholesterol is the principal sterol of all higher animals required to build and maintain membranes.

2019, 11;10(1):4621

S5288

Estropipate

Estropipate (Piperazine estrone sulfate, Estrone sulfate piperazine salt, Pipestrone) is a natural estrogenic substance composed of estrone sulfate and piperazine and is used mainly in menopausal hormone therapy in the treatment of menopausal symptoms.

S4046

Estradiol Cypionate

Estradiol cypionate is the 17 β-cyclopentylpropinate ester of estradiol, which inhibits ET-1 synthesis via estrogen receptor.

2016, 12(9):1593-613

S4638

Desogestrel

Desogestrel (Cerazette, Desogen, Desogestrelum, Org-2969) is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents.

S3657

Promestriene

Promestriene (3-propyl ethyl, 17B-methyl estradiol) is a synthetic estrogen analog that has been reported to significantly improve the symptoms of vaginal atrophy caused by estrogen deprivation in topical application.

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.

S1858

Dienestrol

Dienestrol(Restrol) is a synthetic, non-steroidal estrogen. It is an estrogen receptor agonist.

S4883

Lynestrenol

Lynestrenol (Ethinylestrenol) is a synthetic progestational hormone, an agonist of the progesterone receptor and has weak androgenic and estrogenic activity.

S3635

Medroxyprogesterone

Medroxyprogesterone (MP) is a synthetic pregnane steroid and a derivative of progesterone. It is a potent progesterone receptor agonist.

S4674

Hydroxyprogesterone caproate

Hydroxyprogesterone Caproate (17α-Hydroxyprogesterone hexanoate, 17α-Hydroxyprogesterone caproate) is a synthetic progestational agent. It binds to and activates nuclear progesterone receptors in the reproductive system and inhibits ovulation and an alteration in the cervical mucus and endometrium.

S3671

Quinestrol

Quinestrol (Ethinylestradiol 3-cyclopentyl ether, EE2CPE, W-3566) is a synthetic, steroidal estrogen which is used in hormone replacement therapy and occasionally to treat breast cancer and prostate cancer.

S0407

XCT790

XCT-790 (Compound 12) is a potent and selective inverse agonist for estrogen-related receptor α (ERRα) with IC50 of 0.37 μM. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ. XCT-790 (Compound 12) significantly inhibits in vivo tumor growth and angiogenesis, and induces apoptosis.

S4507

17-Hydroxyprogesterone

17-Hydroxyprogesterone (17-OHP) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.

S4673

Etonogestrel

Etonogestrel (Implanon, Nexplanon, 3-Oxodesogestrel, 3-keto-Desogestrel) is a synthetic form of the naturally occurring female sex hormone progesterone. It binds to the cytoplasmic progesterone receptors in the reproductive system and subsequently activates progesterone receptor mediated gene expression.

S7828

Licochalcone A

Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.

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.

S3160

Ethynodiol diacetate

Ethynodiol diacetate (8080 CB) is one of the first synthetic progestogens used in contraceptive pills.

S2611

Ethisterone

Ethisterone is a progestogen hormone being considered to treat prostate cancer.

S5469

Bavachin

Bavachin (Corylifolin) is a phytoestrogen purified from natural herbal plants such as Psoralea corylifolia. It acts as a weak phytoestrogen by binding and activating the ER.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1972

Tamoxifen Citrate

Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.

2021, 10.1021/acsbiomaterials.0c01803

2021, 21(1):4

2020, S1742-7061(20)30695-4

S1227

Raloxifene HCl

Raloxifene (LY156758, Keoxifene) HCl a selective and orally active estrogen receptor modulator (SERM), which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.

2021, 10.1038/s41589-021-00751-4

2020, 1;AAC.00289-20

2019, 75(6):1103-1116.e9

S8956

(Z)-4-Hydroxytamoxifen

(Z)-4-Hydroxytamoxifen ((Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen) is a selective modulator of estrogen receptor (SERM) with IC50 of 3.3 nM for the [3H]oestradiol binding to oestrogen receptor.

S1776

Toremifene Citrate

Toremifene Citrate (NSC 613680) is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer.

2020, 2020/9/20.4.7.30734

2019, 93(8)

2019, 13(7):e0007595

S2128

Bazedoxifene HCl

Bazedoxifene HCl is a novel, non-steroidal, indole-based estrogen receptor modulator (SERM) binding to both ERα and ERβ with IC50 of 23 nM and 89 nM, respectively.

2021, 10.1038/s41589-021-00751-4

2020, 7 pii: molcanther

2020, 10.1007/s10549-020-05575-9

S2561

Clomifene citrate

Clomifene Citrate (NSC 35770) is a selective estrogen receptor modulator, used in the treatment of ovulation induction.

2020, 19;20:58

2020, 10.1007/s13577-020-00425-8

2020, 10.1007/s13577-020-00420-z

S3081

Ulipristal acetate

Ulipristal acetate (CDB-2914) is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.

2019, 104(12):6256-6264

2017, 50(5)

S1914

Pregnenolone

Pregnenolone is an endogenous steroid hormone, used in the treatment of fatigue, Alzheimer’s disease, trauma and injuries.

2019, 42(10):1833-1841

2018, 32(6):996-1003

S2167

Bazedoxifene Acetate

Bazedoxifene Acetate (WAY-140424, TSE-424) is a third generation selective estrogen receptor modulator (SERM).

2021, 10.1038/s41589-021-00751-4

2020, 7 pii: molcanther

2019, 11(4):e9539

S0503

Estrogen receptor modulator 1

Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM) with pIC50 of 0.46. Estrogen receptor modulator 1 exhibits potential anti-tumor activity.

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.

S4629

Chlorotrianisene

Chlorotrianisene (tri-p-anisylchloroethylene, TACE, CTA) is a synthetic, non-steroidal estrogen. It is a selective estrogen receptor modulator.

S7827

4-Hydroxytamoxifen (Afimoxifene)

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

2021, 21(1):4

2021, 23(1):26

2020, 7(20):2000157

S2301

Genistin (Genistoside)

Genistin (Genistoside, Genistine, Genistein 7-glucoside, Genistein glucoside) is an isoflavone found in a number of dietary plants like soy and kudzu. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of Estrogen Receptor α (ERα) signaling pathway.

S2314

Kaempferol

Kaempferol (Robigenin), a natural flavonol, functions as an ERRα and ERRγ inverse agonist. It inhibits topoisomerase I catalyzed DNA religation and may also inhibit the activity of fatty acid synthase.

2020, 12(12):8007-8018

2020, 12(12):8007-8018

2020, 21(14):5025

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.

2021, 10.1038/s41589-021-00751-4

2020, 10.1002/dta.2917

S9122

Tectorigenin

Tectorigenin (TEC) is an isoflavone isolated from various medicinal plants, such as Pueraria thunbergiana Benth, Belamcanda chinensis, and Iris unguicularis. It has been reported to exert pharmacological actions, including antitumor and antibacterial effects, free radical neutralization, and selective estrogen receptor modulation.

S1238

Tamoxifen

Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis.

2021, 12(4):329

2020, S0092-8674(20)31394-5

2020, 13(663)eaax7119

S4285

Ospemifene

Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.

S5393

Cyclofenil

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

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S5219

Allylestrenol

Allylestrenol is an orally active progestagen of the 19-nortestosterone series resembling progesterone.

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.

S1251

Dienogest

Dienogest (STS 557) is an orally active synthetic progesterone, used for contraception and the treatment of endometriosis.

S1376

Gestodene

Gestodene (SH B 331) is a progestogen hormonal contraceptive.

S1377

Drospirenone

Drospirenone (ZK 3059) is a synthetic progestin that is an analog to spironolactone.

2020, 1(2):235-248

2015, 13(10):1918-24

S1665

Estrone

Estrone is an estrogenic hormone.

2019, 75(6):1103-1116.e9