GLPBio

Estrone

Catalog No.: GC14385Purity:>98.00%Synonyms: E1
COASDSData Sheet
Estrone is one of the three major endogenous estrogens, the others being estradiol and estriol.

Products are for research use only. Not for human use. We do not sell to patients.

Estrone
Cas No.: 53-16-7
10mM (in 1mL DMSO)In Stock
$35.00
1
500mgIn Stock
$28.00
1
1gIn Stock
$35.00
1
5gIn Stock
$57.00
1
10gIn Stock
$78.00
1
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Description

Estrone is one of the three major endogenous estrogens, the others being estradiol and estriol[1]. Estrone is synthesized from cholesterol and is primarily secreted by the gonads, but can also be formed by adrenal androgens in adipose tissue[2]. Estrone is an agonist of the estrogen receptor[3]. Estrone can effectively activate multiple signaling and functional responses in pituitary cells at low physiological concentrations[4].

In vitro, treatment of human endothelial colony-forming cells (hECFCs) with Estrone (0-1µM) for 24h significantly promoted cell proliferation at concentrations of 1nM and 10nM, and inhibited proliferation at a concentration of 1µM[5]. Treatment of bone progenitor cells with Estrone (10nM) upregulated the expression of estrogen receptor α (ER-α) and estrogen receptor β (ER-β), but downregulated the expression of osteopontin (OPN)[6]. Estrone (10-3-105nM) treated mouse colon cancer MC38 cells for 24-72h inhibited cell growth in a dose- and time-dependent manner[7].

In vivo, subcutaneous injection of Estrone (0.5mg/kg) in rats with traumatic brain injury reduced cortical lesion volume and neuronal damage, reduced the level of TUNEL-positive staining in the cerebral cortex, reduced the number of TUNEL-positive cells in the corpus callosum, and reduced the cortical level of β-amyloid protein after brain injury[8].

References:
[1] Bennink H J T C. Are all estrogens the same?[J]. Maturitas, 2004, 47(4): 269-275.
[2] Tchernof A, Mansour M F, Pelletier M, et al. Updated survey of the steroid-converting enzymes in human adipose tissues[J]. The Journal of steroid biochemistry and molecular biology, 2015, 147: 56-69.
[3] Eyster K M. The estrogen receptors: an overview from different perspectives[J]. Estrogen Receptors: Methods and Protocols, 2016: 1-10.
[4] Watson C S, Jeng Y J, Kochukov M Y. Nongenomic actions of estradiol compared with estrone and estriol in pituitary tumor cell signaling and proliferation[J]. The FASEB Journal, 2008, 22(9): 3328.
[5] Ivory A, Greene A S. Distinct roles of estrone and estradiol in endothelial colony‐forming cells[J]. Physiological Reports, 2023, 11(19): e15818.
[6] Park J B. Effects of low doses of estrone on the proliferation, differentiation and mineralization of osteoprecursor cells[J]. Experimental and Therapeutic Medicine, 2012, 4(4): 681-684.
[7] Motylewska E, Mełeń-Mucha G. Estrone and progesterone inhibit the growth of murine MC38 colon cancer line[J]. The Journal of steroid biochemistry and molecular biology, 2009, 113(1-2): 75-79.
[8] Gatson J W, Liu M M, Abdelfattah K, et al. Estrone is neuroprotective in rats after traumatic brain injury[J]. Journal of neurotrauma, 2012, 29(12): 2209-2219.

Protocol

Cell experiment [1]:

Cell lines

Human endothelial colony-forming cells (hECFCs)

Preparation Method

5×104 serum starved hECFCs were seeded into 24 wells plates and incubated with IncuCyte® NucLight Rapid Red Reagent for nuclear labeling. Celprogen media with serum and antibiotics was supplemented with the desired treatment. Treatment groups included: Estrone, estradiol, or 1 to 1 ratio combination of Estrone/estradiol at 0nM (medium control), 1nM, 10nM, 100nM, and 1µM. The hECFCs were then incubated for 24h during which the cells were imaged in the IncuCyte SX5 Live-Cell Analysis System (Sartorius). Cell number was then quantified and presented as percentage of control.

Reaction Conditions

1nM, 10nM, 100nM, 1µM; 24h

Applications

The effect of Estrone on hECFC proliferation was biphasic with only exposures of 1nM and 10nM resulting in significant increases in hECFC proliferation. Estrone exposure at 1μM resulted in attenuated proliferation and resulted in a significantly lower hECFC cell number than control.
Animal experiment [2]:

Animal models

Sprague-Dawley rats

Preparation Method

The Benchmark Stereotaxic Impactor was used to administer severe TBI in rats. An incision was made to expose the skull, and the craniotomy procedure was performed. Following the craniotomy procedure, a cortical contusion was delivered to the right hemisphere via a vertically-directed pneumatic cylinder. The skin was closed with surgical wound clips. At 30min following brain injury, the animals were treated subcutaneously with Estrone (0.5mg/kg) or vehicle (corn oil). Control and sham (craniotomy only) animals were also included as controls. The animals were monitored for pain every 6h for the first 24h, and once a day thereafter. At 72h following injury, the animals were perfusedintracardially with 0.9% saline followed by 10% phosphate-buffered formalin. The whole brain was removed, sliced, and stained for TUNEL-positive cells.

Dosage form

0.5mg/kg; s.c.

Applications

Estrone decreased cortical lesion volume and neuronal injury, and it reduced cerebral cortical levels of TUNEL-positive staining, and decreased numbers of TUNEL-positive cells in the corpus callosum. 

References:
[1]Ivory A, Greene A S. Distinct roles of estrone and estradiol in endothelial colony?forming cells[J]. Physiological Reports, 2023, 11(19): e15818.
[2]Gatson J W, Liu M M, Abdelfattah K, et al. Estrone is neuroprotective in rats after traumatic brain injury[J]. Journal of neurotrauma, 2012, 29(12): 2209-2219.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
53-16-7
Synonyms
E1
Chemical Name
(8R,9S,13S,14S)-3-hydroxy-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-one
SMILES
CC12CCC3C(C1CCC2=O)CCC4=C3C=CC(=C4)O
Molecular Formula
C18H22O2
Molecular Weight
270.37
Solubility
≥ 9.75 mg/mL in DMSO, ≥ 9.2 mg/mL in EtOH with ultrasonic and warming
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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