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product name Hexestrol


Description: Hexestrol (also known as Bibenzyl) binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively. 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.

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



Molecular Weight (MW)

270.37 
Formula

C18H22O2 
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
Synonyms

Bibenzyl 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19417594

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.


Kinase Assay:


Cell Assay

In Vivo Hexestrol 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 model Mice
Formulation & Dosage Dissolved 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. 

AVE 0992 (sodium salt)

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Author: Sodium channel