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      Hexestrol (HSDB 2149)
      Hexestrol (HSDB 2149)

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V1731
      CAS #: 84-16-2Purity ≥98%

      Description: Hexestrol (formerly HSDB2149; HSDB-2149; Cycloestrol; Hexoestrol; Erythrohexestrol; Sinestrol) is a synthetic ER (estrogen receptor) agonist which binds to ERα and ERβ with EC50s of 0.07 nM and 0.175 nM, respectively. It also acts as a microtubule polymerization inhibitor.

      References: Eur J Med Chem. 2009 Sep;44(9):3412-24; Ann N Y Acad Sci. 2004 Dec;1028:247-57.

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      Molecular Weight (MW)270.37 
      FormulaC18H22O2 
      CAS No.84-16-2 
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO: 42 mg/mL (155.3 mM) 
      Water: <1 mg/mL
      Ethanol: 42 mg/mL (155.3 mM)  
      Solubility (In vivo)30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
      SynonymsHSDB 2149; Cycloestrol; Erythrohexestrol; HSDB2149; HSDB-2149; Hexoestrol; Sinestrol


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      In Vitro

      In vitro activity: Hexestrol binds to ERα with EC50 of 0.07 nM and to ERβ with EC50 of 0.175 nM. Hexestrol inhibits activity of AKR1B13 with IC50 of 3.2 μM. Hexestrol inhibits the d-galactose dehydrogenase activity of thermophilus aldose 1-dehydrogenase with IC50 of 0.063 mM. Hexestrol inhibits the dehydrogenase activity of AKR1C20 towards 10 μM 4-androsten-3α-o1-17-one with IC50 values of 2.7 μM. Hexestrol inhibits 17HSD5 with IC50 of 30 μM, and inhibits TBER1 with IC50 of 0.8 μM. Hexestrol reacts with DNA through the catechol quinone, thus can be a carcinogen.

      In VivoHexestrol administered intraperitoneally at dose of 6 mg/kg may decrease ovulation in mice, as evident by smaller ovaries and decreased luteal bodies and oocytes. 
      Animal modelMice
      Formulation & DosageDissolved in saline; 3 mg/kg and 6 mg/kg; i.p. injection
      References

      Eur J Med Chem. 2009 Sep;44(9):3412-24; Ann N Y Acad Sci. 2004 Dec;1028:247-57. 

      These protocols are for reference only. InvivoChem does not independently validate these methods.

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