1. Metabolic Enzyme/Protease
  2. 5 alpha Reductase
    Endogenous Metabolite
  3. Alpha-Estradiol

Alpha-Estradiol (Synonyms: Alfatradiol; Epiestradiol; Epiestrol)

Cat. No.: HY-B0141A Purity: 99.46%
Handling Instructions

Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.

For research use only. We do not sell to patients.

Alpha-Estradiol Chemical Structure

Alpha-Estradiol Chemical Structure

CAS No. : 57-91-0

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.

IC50 & Target

Human Endogenous Metabolite

 

In Vitro

Alpha-Estradiol (17 alpha-Estradiol) is a 5α-reductase inhibitor, and inhibits testosterone metabolism catalyzed by 5 alpha-reductase[1]. Alpha-Estradiol (17 Alpha-estradiol, 10 μM) attenuates LPS-induced inflammatory markers in both C57BL/6J male and female mouse embryonic fibroblast (MEF) cells, primary pre-adipocytes and differentiated 3T3-L1 adipocytes in an ERα-dependent manner, and such effects are through decreased NFκB-p65 and increased ERα protein expression[2].

In Vivo

Alpha-Estradiol (17-alpha-estradiol, 0.01, 0.1, 1 μg) significantly reduces the percentage of central avascular/total retina area of the mouse pups. Alpha-Estradiol (1 μg) markedly decreasesmalondialdehyde (MDA) levels on postnatal days (PND) 9, 13, and 17 in retinas of hyperoxia-exposed pups. Alpha-Estradiol (1 μg) also decreases the number of NADPH-oxidase-positive cells, NADPH oxidase concentration and activity in retinas of the pups. In the 1.0-μg Alpha-Estradiol-treated pups, VEGF retinal concentrations are high on PND 9 but lower on PND 14 and 17. The best effect in retinas of 1.0-μg Alpha-Estradiol-treated pups is partly reversed by ICI182780 on PND 14 and 17[3].

Molecular Weight

272.38

Formula

C₁₈H₂₄O₂

CAS No.

57-91-0

SMILES

C[[email protected]@]12[[email protected]](O)CC[[email protected]@]1([H])[[email protected]]3([H])CCC4=C(C=CC(O)=C4)[[email protected]@]3([H])CC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (367.13 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.18 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.18 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

Mouse embryonic fibroblast (MEF) cells are treated for the indicated time with Alpha-Estradiol (17 α-E2) or 17 β-E2 at 10 μM concentration. Inflammation is induced by LPS at a concentration of 10 ng/mL either alone or in combination with the respective estrogen[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Newborn mice are randomLy assigned to six groups according to the kind of treatment: room air with vehicle injection (control, group 1), hyperoxia with vehicle injection (control, group 2), hyperoxia with 0.01 μg Alpha-Estradiol injection (group 3), hyperoxia with 0.1 μg Alpha-Estradiol injection (group 4), hyperoxia with 1.0 μg Alpha-Estradiol injection (group 5), and hyperoxia with 1.0 μg Alpha-Estradiol and 10.0 μg ICI182780 injection (antagonist of estrogen receptor α and β) (group 6). The pups receive daily subcutaneous injections of either Alpha-Estradiol in vehicle [dissolved in ethanol and diluted in 0.05 mL/mouse of phosphate-buffered saline (PBS)] or vehicle alone from postnatal days (PND) 7-16. On PND 7, the pups in the hyperoxia and Alpha-Estradiol-treatment groups are exposed to hyperoxia (75 ± 2 % O2) for 5 days (PND 7-12) and then returned to normoxia (room air) for 5 days, along with the nursing mothers, whereas pups in the normoxia group are kept in normoxia from PND 7-17. The pups are humanely euthanized on PND 9, 13 (14), and 17[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

Alpha-EstradiolAlfatradiolEpiestradiolEpiestrol5 alpha ReductaseEndogenous Metabolite5α-reductaseInhibitorinhibitorinhibit

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