in vivo/in vitro におけるエストラジオールの挙動を観察

 

 

 

 

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Description

Estradiol Glow is the ovarian steroid hormone 17-ß-Estradiol labeled with a novel low molecular weight orange/red fluorophor thus retaining it´s chemical properties and it´s biological activity. This allows for a wide range of applications including

• analysis of in vivo and in vitro steroid uptake in real time

• monitoring of intracellular and subcellular steroid transport

• studies on steroid-binding proteins

• use as tracer for steroid immunoassays (to replace isotopes or enzymes)

• photodynamic elimination of estrogen sensitive tissues and cells in experimental settings with possible future clinical implications

Background

Identification of steroid sensitive cells in target tissues has so far been attempted with either radio labelled hormones and autoradiography or with in situ hybridization and immuno-histochemistry for receptor proteins. Numerous studies have been performed with steroid hormones labelled with either enzymes, fluorophors or immunogenic markers, all resulting in loss of biological properties and hormonal function. Estradiol Glow is 17-ß-estradiol, labelled in a novel way with a low molecular weight biocompatible fluorophor, thus retaining biological activity of the ovarian hormone. Systemic injections into experimental animals revealed accumulation of the fluorescent steroid in nuclei of known estrogen target tissues, including the brain.

Estradiol Glow allows new insights into cellular uptake, intracellular transport and subcellular binding. Mechanisms of rapid steroid actions become transparent on the single cell level.

Structure

 

 

 

 

 

 

Solubility

High: MeOH, EtOH, PrOH, DMSO, DMF

Moderate: acetone, CH₂Cl₂, CH₃Cl, THF

Low: H₂O and aqueous buffer systems (after presolution in DMSO >1 μM)

Insoluble: Et₂O, hydrocarbons such as hexane, heptane, benzene

Molecular formula

C₄₇H₆₇N₂O₂Br

Molecular weight

771.96 g/mol

Form

brownish-red, glassy to waxy powder

Purity

>97% (DC, NMR)

Spectral data

in PBS buffer (pH 7.4): Ex/Em(nm) = 467 /618, μ = 29,000 l/mol∙cm

in ethanol:

Ex/Em(nm) = 501/596, μ = 52,000 l/mol∙cm

 

 

 

 

 

 

 

 

 

Nuclear accumulation of Estradiol glow in rat paraventricular hypothalamic neurons after in vivo i.p. injection. 100 μm vibratome, section of the perfusion fixed brain.

 

 

 

 

 

 

 

 

 

Cytoplasmic and nuclear uptake of estradiol glow in MCF7 breast cancer cell culture.

 

Product Name	Product No.	Size
Estradiol Glow (Fluorescently labeled Estradiol)	PR-958S	100ug
	PR-958L	500ug

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