Estriol (Synonyms: E3, 16α-hydroxy-17β-Estradiol, 1,3,5(10)-Estratriene-3,16α,17β-triol) |
Catalog No.GC12182
One-Click Copy Product Info
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Estriol is an agonist of estrogen receptors (ERα and ERβ) and G protein-coupled receptor 30 (GPR30) antagonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 50-27-1
Sample solution is provided at 25 µL, 10mM.
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Estriol is an agonist of estrogen receptors (ERα and ERβ) and G protein-coupled receptor 30 (GPR30) antagonist [1]. Estriol binds to ERα/ERβ in the nucleus, inducing gene transcription and influencing cell proliferation, differentiation, and other functions [2]. Estriol is used for topical skin anti-aging and potential immunomodulatory treatments [3-4].
In SkBr3 cells, Estriol (1μM; 6d) can block the abnormal proliferation of breast cancer cells by inhibiting the GPR30-dependent signaling pathway [1]. In MDA-MB-231 cells, Estriol (1-80μM; 7d) inhibits 17β-estradiol-stimulated cell proliferation [5]. In myelin basic protein-reactive T cell, Estriol (0-50ng/mL; 16h) treatment showed a dose-dependent inhibitory effect on cell migration [6].
In pentylenetetrazol (PTZ)-kindled epilepsy mouse model, Estriol (0.005mg/kg, 0.01mg/kg; ip; single injection) treatment increases the incidence of epileptic seizures [7]. In a streptozotocin-induced type 1 diabetic mouse model, Estriol (3.5µM; iv; single injection) controls hyperglycemia through hepatic insulin synthesis [8].
References:
[1]. Lappano R, Rosano C, De Marco P, et al. Estriol acts as a GPR30 antagonist in estrogen receptor-negative breast cancer cells[J]. Molecular and cellular endocrinology, 2010, 320(1-2): 162-170.
[2]. Kim S, Liva S M, Dalal M A, et al. Estriol ameliorates autoimmune demyelinating disease: implications for multiple sclerosis[J]. Neurology, 1999, 52(6): 1230-1230.
[3]. Ali E S, Mangold C, Peiris A N. Estriol: emerging clinical benefits[J]. Menopause, 2017, 24(9): 1081-1085.
[4]. Merrill R C. Estriol: a review[J]. Physiological reviews, 1958, 38(3): 463-480.
[5]. Girgert R, Emons G, Gründker C. Inhibition of GPR30 by estriol prevents growth stimulation of triple-negative breast cancer cells by 17β-estradiol[J]. BMC cancer, 2014, 14(1): 935.
[6]. Zang Y C Q, Halder J B, Hong J, et al. Regulatory effects of estriol on T cell migration and cytokine profile: inhibition of transcription factor NF-κB[J]. Journal of neuroimmunology, 2002, 124(1-2): 106-114.
[7]. Ahmad A, Vohora D. Proconvulsant effects of estriol, the third estrogen, in the mouse PTZ-kindling model[J]. Neurological Sciences, 2014, 35(10): 1561-1566.
[8]. Bhattacharya S, Bank S, Maiti S, et al. The control of hyperglycemia by estriol and progesterone in alloxan induced type I diabetes mellitus mice model through hepatic insulin synthesis[J]. International Journal of Biomedical Science: IJBS, 2014, 10(1): 8.
| Cell experiment [1]: | |
Cell lines | SkBr3 cells |
Preparation Method | SkBr3 breast cancer cells were seeded in 96-well plates at a density of 10,000 cells per well. After adherence, they were cultured in 2.5% delipidated FBS and treated with the GPR30 agonist G-1 (100nM) and/or Estriol (E3, 1μM). Incubation was continued for 6 days, with fresh medium and treatment every 2 days. After treatment, cell proliferation activity was assessed using the MTT assay. |
Reaction Conditions | 1μM; 6d |
Applications | Estriol can block the abnormal proliferation of breast cancer cells by inhibiting the GPR30-dependent signaling pathway. |
| Animal experiment [2]: | |
Animal models | Pentylenetetrazol (PTZ)-kindled epilepsy mouse model |
Preparation Method | Swiss Albino mice weighing between 25 and 35g were used. They were housed in polypropylene cages and maintained at 25–30℃ and 50–55 % humidity in a natural light/dark cycle. Estriol was dissolved in DMSO and administered in doses of 0.005 and 0.01mg/kg, ip. Control group received DMSO as vehicle. Clomiphene was dissolved in distilled water and administered intraperitoneally at dose of 0.9mg/kg. Diazepam was taken as standard and was given at 3mg/kg. Pentylenetetrazole (PTZ) was administered 1h after Estriol and clomiphene treatment and 1.5h after diazepam treatment in the respective groups. |
Dosage form | 0.005mg/kg, 0.01mg/kg; ip; single injection |
Applications | Estriol treatment increases the incidence of epileptic seizures in mice. |
References: | |
| Cas No. | 50-27-1 | SDF | |
| Synonyms | E3, 16α-hydroxy-17β-Estradiol, 1,3,5(10)-Estratriene-3,16α,17β-triol | ||
| Chemical Name | (8R,9S,13S,14S,16R,17R)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,16,17-triol | ||
| Canonical SMILES | CC12CCC3C(C1CC(C2O)O)CCC4=C3C=CC(=C4)O | ||
| Formula | C18H24O3 | M.Wt | 288.39 |
| Solubility | ≥ 9.25mg/mL in DMSO | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4675 mL | 17.3376 mL | 34.6753 mL |
| 5 mM | 693.5 μL | 3.4675 mL | 6.9351 mL |
| 10 mM | 346.8 μL | 1.7338 mL | 3.4675 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)