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Cat. No. M3333
Hexestrol Structure


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50mg USD 45  USD50 In stock
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Quality Control
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).

Cell Experiment
Cell lines
Preparation method
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 270.37
Formula C18H22O2
CAS Number 84-16-2
Purity 99.90%
Solubility DMSO 40 mg/mL
Storage at -20°C
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Keywords: Hexestrol, Bibenzyl supplier, Estrogen Receptor, inhibitors

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