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Hexestrol

Cat. No. M3333
Hexestrol Structure
Synonym:

Bibenzyl

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50mg USD 50  USD50 In stock
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Quality Control & Documentation
Biological Activity

Hexestrol (Bibenzyl) is a novel type of 17β-hydroxysteroid dehydrogenase, AKR1C1and AKR1C2 potent inhibitor with IC50 of 0.8, 9.5, 2.8 µM, respectively and exhibits strong affinity for estrogen receptors. It is a synthetic estrogen that has been used as a hormonal antineoplastic agent. Rat liver contains two cytosolic enzymes (TBER1 and TBER2). TBER1 represents a novel type of 17β-hydroxysteroid dehydrogenase with unique catalytic properties and tissue distribution.. The recombinant TBER1 efficiently oxidized 17β-hydroxysteroids and xenobiotic alicyclic alcohols using NAD+ as the preferred coenzyme at pH 7.4, and showed low activity towards 20α- and 3α-hydroxysteroids, and 9-hydroxyprostaglandins. The enzyme was potently inhibited by diethylstilbestrol, hexestrol and zearalenone. Rat 17HSD5 differed from TBER1 in inhibitor sensitivity. The inhibitory potencies of diethylstilbestrol (IC50 = 7.5 µM), hexestrol (IC50 = 30 µM), and zearalenone (IC50 = 36 µM) for 17HSD5 were lower than those for TBER1 (the respective IC50 values were 1.7, 0.8 and 7.5 µM).

Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models adult mice aged 90-120 days
Formulation Saline
Dosages 3 mg/kg and 6 mg/kg
Administration administered intraperitoneally once daily for 30 days
Chemical Information
Molecular Weight 270.37
Formula C18H22O2
CAS Number 84-16-2
Solubility (25°C) DMSO 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Karan Chaudhary, et al. Ruthenium oxide nanoparticles immobilized over Citrus limetta waste derived carbon material for electrochemical detection of hexestrol

[2] Iraida G Syasina, et al. Hexestrol- and nonylphenol-induced differential vitellogenin synthesis in female and male barfin plaice Liopsetta pinnifasciata

[3] K J Karnaky. Hexestrol choice estrogen

[4] J G Liehr, et al. Carcinogenicity and metabolic activation of hexestrol

[5] Y Inamori, et al. Biological activities of hexestrol

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Keywords: Hexestrol, Bibenzyl supplier, Estrogen Receptor, inhibitors, activators


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