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Alpha-Estradiol, an endogenous estrogen receptor ligand, is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
| ln Vitro |
The 5α-reductase inhibitor 17 alpha-estradiol prevents the metabolism of testosterone that is catalyzed by 5α-reductase [1]. α-Estradiol (17α-estradiol, 10 μM) attenuates LPS-induced inflammatory markers in cells by decreasing NFκB-p65 and upregulating ERα protein expression in C57BL/6J male and female mouse embryonic fibroblast (MEF) cells, primary preadipocytes, and differentiated 3T3-L1 adipocytes in an ERα-dependent manner [2].
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| ln Vivo |
In juvenile rats, α-estradiol (17-α-estradiol, 0.01, 0.1, 1 μg) dramatically decreased the ratio of central avascular/total retinal area. On postnatal days 9, 13, and 17, malondialdehyde (MDA) levels in the retina of puppies exposed to hyperoxia were dramatically decreased by 1 μg of α-estradiol. In the retina of puppies, α-estradiol (1 μg) likewise decreased the quantity, concentration, and activity of NADPH oxidase-positive cells. Puppies given 1.0 μg α-estradiol had higher retinal concentrations of VEGF at PND 9 but decreased amounts at PND 14 and 17. The optimum effect in the retina of puppies treated with 1.0 μg α-estradiol on PND was partially reversed by ICI182780. 14 and 17 [3].
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| References |
[1]. Schriefers H, et al. Inhibition of testosterone metabolism by 17-alpha-estradiol in rat liver slices. Arzneimittelforschung. 1991 Nov;41(11):1186-9.
[2]. Santos RS, et al. The effects of 17 alpha-estradiol to inhibit inflammation in vitro. Biol Sex Differ. 2017 Sep 6;8:30. [3]. Zhang HB, et al. 17-Alpha-estradiol ameliorating oxygen-induced retinopathy in a murine model. Jpn J Ophthalmol. 2012 Jul;56(4):407-15 |
| Molecular Formula |
C₁₈H₂₄O₂
|
|---|---|
| Molecular Weight |
272.38
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| CAS # |
57-91-0
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| SMILES |
C[C@@]12[C@H](O)CC[C@@]1([H])[C@]3([H])CCC4=C(C=CC(O)=C4)[C@@]3([H])CC2
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| Synonyms |
Alfatradiol Epiestradiol Epiestrol
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~229.46 mM)
Ethanol : ~11.11 mg/mL (~40.79 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 0.58 mg/mL (2.13 mM) in 5% EtOH + 95% PBS (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6713 mL | 18.3567 mL | 36.7134 mL | |
| 5 mM | 0.7343 mL | 3.6713 mL | 7.3427 mL | |
| 10 mM | 0.3671 mL | 1.8357 mL | 3.6713 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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