Estradiol (E2) is a naturally occurring steroidal sex hormone that is essential for female fertility and maintenance of secondary sexual characteristics. Estradiol upregulates IL-6 expression through estrogen receptor beta (ERβ).

ERα:22-28 nM, ERα (mouse):22-28 nM, ERα (human):22-28 nM

Method: Human lens epithelial cells HLEC were treated with Estradiol (0.001-10 μM) for 24 h. Cell viability was measured using the MTT.
Result: The number of viable cells was significantly reduced in the presence of 10 μM Estradiol. ^[1]
Method: Human breast cancer cells MB231 were treated with Estradiol (100 nM) for 24 h. Cell motility was detected using scratch/wound healing assay and transwell assay.
Result: Estradiol treatment reduced the migration and invasion of MB231 cells. ^[2]

Method: To assay in vivo activity, Estradiol (0.2 mg/kg) and progesterone (5-20 mg/kg) were administered intraperitoneally as a single injection to ovariectomized C57BL/6 female mice.
Result: Mice receiving Estradiol alone or Estradiol plus 10-20 mg/kg progesterone showed significantly enhanced memory for new objects. ^[3]
Method: To assay in vivo activity, Estradiol (0.2 mg/kg) was administered by gavage to ovariectomized C57BL/6 female mice once daily for two weeks.
Result: Long-term activation of ERβ reduced hot flash-like symptoms and enhanced spatial and object recognition memory in ovariectomized mice. ^[4]

Estradiol is dissolved in 0.01% ethanol. Briefly, B9 cells (5×103/well of a 96-well plate) are cultured with a series of dilutions of the supernatants in a final volume of 100 mL of RPMI 1640, supplemented with 5×10-5mol/Lof 2-mercaptoethanol, 10% FBS, 100 U/mL penicillin, and 100 μg/mL streptomycin in flat-bottom microtiter plates. After 42 h, 0.5 μCi of [3H]thymidine is added. 6 h later, the cells are harvested and the radioactivity incorporated is determined. IL-6 is quantitated from a standard curve set up with known amounts of recombinant human or mouse IL-6. The anti-IL-6 monoclonal antibody completely inhibited the ability of the B9 cells to proliferate in response to recombinant mouse IL-6. In addition, we determined that B9 cells do not proliferate in response to IL-I or TNF, and that antibodies to these two cytokines did not affect the cell proliferation in response to IL-6. Further, it is established that neither Estradiol (17β-estradiol), nor the 0.01% ethanol used as vehicle in these experiments, has any effect on the bioassay.

H2O: <1 mg/mL (insoluble)

Ethanol: 20.40 mg/mL (74.89 mM), Sonication is recommended.

DMSO: 250.00 mg/mL (917.83 mM), Sonication is recommended.

10% DMSO+90% Saline: < 10 mg/mL (36.71 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.73 mg/mL (10.02 mM), Suspension.

10% DMSO+40% PEG300+ 5% Tween 80 + 45% Saline: 10.00 mg/mL (36.71 mM), Suspension.