|S1191||Fulvestrant||<1 mg/mL||100 mg/mL||100 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|
|S1709||Estradiol||<1 mg/mL||54 mg/mL||5 mg/mL|
|S2606||Mifepristone||<1 mg/mL||85 mg/mL||19 mg/mL|
|S8372||AZD9496||<1 mg/mL||88 mg/mL||88 mg/mL|
|S1776||Toremifene Citrate||<1 mg/mL||100 mg/mL||<1 mg/mL|
|S1251||Dienogest||<1 mg/mL||62 mg/mL||<1 mg/mL|
|S2128||Bazedoxifene HCl||<1 mg/mL||101 mg/mL||<1 mg/mL|
|S2604||Dehydroepiandrosterone (DHEA)||<1 mg/mL||57 mg/mL||57 mg/mL|
|S1376||Gestodene||<1 mg/mL||62 mg/mL||8 mg/mL|
|S2561||Clomifene citrate||<1 mg/mL||120 mg/mL||11 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|
|S1377||Drospirenone||<1 mg/mL||73 mg/mL||11 mg/mL|
|S1705||Progesterone||<1 mg/mL||22 mg/mL||63 mg/mL|
|S1304||Megestrol Acetate||<1 mg/mL||33 mg/mL||15 mg/mL|
|S3081||Ulipristal||<1 mg/mL||83 mg/mL||14 mg/mL|
|S2466||Estriol||<1 mg/mL||57 mg/mL||10 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|
|S1914||Pregnenolone||<1 mg/mL||22 mg/mL||22 mg/mL|
|S1665||Estrone||<1 mg/mL||54 mg/mL||<1 mg/mL|
|S2125||Mestranol||<1 mg/mL||15 mg/mL||25 mg/mL|
|S2167||Bazedoxifene Acetate||<1 mg/mL||100 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|
|S4629||Chlorotrianisene||<1 mg/mL||76 mg/mL||<1 mg/mL|
|S7827||4-Hydroxytamoxifen||<1 mg/mL||77 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|
|S2314||Kaempferol||<1 mg/mL||57 mg/mL||3 mg/mL|
|S4674||Hydroxyprogesterone caproate||<1 mg/mL||85 mg/mL||85 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|
|S1238||Tamoxifen||<1 mg/mL||74 mg/mL||74 mg/mL|
|S7839||Endoxifen HCl||<1 mg/mL||74 mg/mL||74 mg/mL|
|S3160||Ethynodiol diacetate||77 mg/mL||77 mg/mL||<1 mg/mL|
|S4285||Ospemifene||<1 mg/mL||75 mg/mL||71 mg/mL|
|S2611||Ethisterone||<1 mg/mL||0.05 mg/mL||<1 mg/mL|
- Estrogen/progestogen Receptor阻害剤(44)
- 新Estrogen/progestogen Receptor製品
Fulvestrant is a Synthetic estrogen receptor antagonist(SERD)
PTPH1 confers breast cancer cell sensitivity to fulvestrant. E and F, PTPH1 overexpression increases the growth inhibition by fulvestrant. PTPH1 was overexpressed by a Tet-on system or a stable transfection, and resultant cells were incubated with fulvestrant as indicated for about 2 weeks. Colony formed was stained and counted. Results shown are normalized to its own solvent control of Vector and PTPH1-overexpressed cells, respectively (means ± SD; n = 3–5) with insets showing PTPH1 overexpression. *, versus vector or no Tet cells for E and F.
Effects of DPN, LY500307, Raloxifene and Tamoxifen on cell viability in BSO-treated FRDA fibroblasts. BSO concentration was 1 mM and all steroid concentrations were 100 nM. Depicted are mean ± SD for n= 8 per group. * indicated p<0.05 versus BSO alone-treated cells.
Raloxifene HCl is estrogen antagonists, inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.
Estradiol is the predominant sex hormone.
Mifepristoneは非常に活発な拮抗プロゲステロン受容体と砂糖皮質ホルモン受容体、IC50がそれぞれ 0.2 nM と 2.6 nM になる。
Myogenic differentiation assay to determine the GR specificity of DEX by using RU-486 (10 uM). Immunofluorescence detection of MyHC (red) and DAPI counterstaining of nuclei (blue) was used to detect myotubes. The scale bar is 50 um.
Toremifene Citrate is an oral selective estrogen receptor modulator (SERM) which helps oppose the actions of estrogen in the body.
D: Marginal degradation of MGMT in MCF7 cells treated with toremifene, a SERM. MGMT: O6-methylguanine DNA-methyltransferase; C: control.
Dienogest is an orally active synthetic progesterone (or progestin).
Entecavir monohydrate (Baraclude) is a reverse transcription, DNA replication and transcription inhibitor with an IC50 of about 0.5 nM.
Dehydroepiandrosterone(DHEA) is a 19-carbon endogenous natural steroid hormone.
Gestodene is a progestogen hormonal contraceptive.
Clomifene citrate is a selective estrogen receptor modulator.
(a) Inhibitory activities of IDH1R132H enzyme lead to decreased production of D-2HG in IDH1R132H mutant HT1080 cells after treatment with clomifene for 48 h, and D-2HG was measured by LC/MS method. (b) HT1080 cells were treated for 24 h in the different concentrations of clomifene and then processed for FACS by using Annexin V/propidium iodide staining. (c) Treatment of clomifene significantly reduced methylation levels of histone lysine residues in HT1080 cells. All data are the average of results from triplicate experiments.
Equol is an isoflavandiol metabolized from daidzein by bacterial flora in the intestines.
Levonorgestrel(Levonelle) is a synthetic progestogen used as an active ingredient in some hormonal contraceptives.
Medroxyprogesterone acetate (MPA) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding.
The analgesic effect of koumine was reversed in sciatic nerve chronic constriction injury rats by intrathecal treatment with medroxyprogesterone acetate. Medroxyprogesterone acetate (MPA) or dimethyl sulfoxide (DMSO, vehicle) was administered via an intrathecal catheter 10 days after sciatic nerve chronic constriction injury (CCI) surgery. After 30 min, koumine (7 mg kg−1 bw) or normal saline (NS) was administered by subcutaneous (s.c.) injection. The mechanical withdrawal threshold (MWT) of the hind paws was measured 1 h after completion of the drug or vehicle administration. The data are presented as the mean ± SEM (n = 6 per group) and were analyzed by one-way ANOVA followed by Bonferroni post hoc test at each time point. *P < 0.05 vs. the DMSO + NS group; # P < 0.05 vs. the DMSO + koumine group.
Hexestrolは、Erα＜/b、ERβと結合しまして、 EC50 がそれぞれ 0.07 nM と 0.175 nMです。
Drospirenone is a synthetic progestin that is an analog to spironolactone.
Progesterone is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species.
SPOP inhibits progesterone-induced S phase entry and Erk1/2 activation. (A) T47D cells were transfected with control or Myc-SPOP constructs. After 24 hr, cells were treated with the vehicle ethanol (EtOH) or progesterone (10 nM) for 24 hr. The cell cycle percentages was determined by PI staining and FACS; (B) T47D cells were transfected with control siRNAs or SPOP-specific siRNAs. After 48 hr, cells were treated and analyzed as in (A); (C) T47D cells were transfected with control or Myc-SPOP constructs. After 24 hr, cells were treated with the vehicle ethanol (EtOH) or progesterone (10 nM) for indicated times. Cell lysates were prepared for WB analyses; (D) T47D cells were transfected with control or SPOP-specific siRNA. After 48 hr, cells were treated and analyzed as in (C).
Megestrol Acetate is a synthetic progesteronal agent with an IC50 of 260 μM for the inhibition of HepG2.
Ulipristal is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.
Diethylstilbestrol, a synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders.
Ethynyl estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.
Estradiol valerate is a synthetic ester used to treat menopausal symptoms and hormone deficiencies.
Pregnenolone is an endogenous steroid hormone for inhibition of M1 receptor- and M3 receptor-mediated currents with IC50 of 11.4 μM and 6.0 μM, respectively.
Estrone is an estrogenic hormone.
Mestranol is the 3-methyl ether of ethinylestradiol. It was the estrogen used in many of the first oral contraceptives.
Bazedoxifene Acetate is a third generation selective estrogen receptor modulator (SERM).
Estradiol benzoate は、人間のマウスおよび鶏ERαにバインドエストラジオールアナログで、IC50 が22-28 nMです。
Altrenogest is a progestogen structurally related to veterinary steroid trenbolone.
CDK4/6 inhibitor resistance promotes diminished ER expression and activity. (a and b) Proliferation of MCF-7 and MR cells in the presence of different concentrations of ICI (a) or 4-hydroxytamoxifen (4-OHT) (b) was measured by the alamarBlue assay and plotted as % inhibition of proliferation against log concentration of inhibitor. Each data point represents the average value±s.d. of six replicates obtained in three independent experiments.
Estradiol cypionate 、エストロゲン受容体によりET-1の合成を阻害するエストラジオールの油溶性17β-cyclopentylpropinateエステルである。
Kaempferol is a natural flavonol, a type of flavonoid, that has been isolated from plant sources.
Total cellular protein was harvested after 8 days and the protein levels of adipogenic factors were measured using western blot analysis with specific antibodies (B).
Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.
E, Analysis of BrCSC viability upon treatment with tamoxifen (tam) and fulvestrant (fulv) at the indicated doses. The experiments were performed in triplicates. ** P<0.01.
Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
Ethynodiol diacetate is one of the first synthetic progestogens used in contraceptive pills.
Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia.
Ethisterone is a progestogen hormone being considered to treat prostate cancer.