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).
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Cell lines | |
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Incubation time |
Animal Experiment | |
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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 |
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 |
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.
[3] K J Karnaky. Hexestrol choice estrogen
[4] J G Liehr, et al. Carcinogenicity and metabolic activation of hexestrol
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