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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 | |
| 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 |
| 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 |
[3] K J Karnaky. Hexestrol choice estrogen
[4] J G Liehr, et al. Carcinogenicity and metabolic activation of hexestrol
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