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Hexestrol

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Chemical Structure| 84-16-2 同义名 : meso-Hexestrol;Bibenzyl;Sinestrol;HSDB 2149;Erythrohexestrol;Cycloestrol;NSC 9894;Hexoestrol
CAS号 : 84-16-2
货号 : A228315
分子式 : C18H22O2
纯度 : 99%
分子量 : 270.366
MDL号 : MFCD00068996
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(388.36 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 46 mg/mL suspension

生物活性
描述 Hexestrol is a estrogen receptor (ER) subtype-selective ligands. Hexestrol binds to ER α and ER β with EC50 of 0.07 nm and 0.175 nm, respectively[3]. Hexestrol inhibited akr1b13 activity with IC50 of 3.2 μ M[4]. Hexestrol inhibited the activity of D-galactose dehydrogenase in 1-Dehydrogenase of Streptococcus thermophilus with IC50 of 0.063 mm[5]. Hexestrol inhibited the dehydrogenase activity of akr1c20, and the IC50 of 10 μ m 4-androsten-3 α - o1-17-one was 2.7 μ M[6]. Hexestrol inhibited 17hsd5 with IC50 of 30 μ m and tber1 with IC50 of 0.8 μ M[7]. In mice treated with hexestrol (6 mg/kg) (Group II), ovaries were smaller than those from the controls but highly vascularized; similar results were obtained in GIV. The anabolic agent hexestrol in a high dose may decrease ovulation in mice[8].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.70mL

0.74mL

0.37mL

18.49mL

3.70mL

1.85mL

36.99mL

7.40mL

3.70mL
参考文献

[1]Waibel M, De Angelis M, et al. Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta. Eur J Med Chem. 2009 Sep;44(9):3412-24.

[2]Endo S, Matsunaga T, et al. Characterization of a rat NADPH-dependent aldo-keto reductase (AKR1B13) induced by oxidative stress. Chem Biol Interact. 2009 Mar 16;178(1-3):151-7.

[3]Waibel M, De Angelis M, Stossi F, Kieser KJ, Carlson KE, Katzenellenbogen BS, Katzenellenbogen JA. Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta. Eur J Med Chem. 2009 Sep;44(9):3412-24

[4]Endo S, Matsunaga T, Mamiya H, Hara A, Kitade Y, Tajima K, El-Kabbani O. Characterization of a rat NADPH-dependent aldo-keto reductase (AKR1B13) induced by oxidative stress. Chem Biol Interact. 2009 Mar 16;178(1-3):151-7

[5]Asada Y, Endo S, Inoue Y, Mamiya H, Hara A, Kunishima N, Matsunaga T. Biochemical and structural characterization of a short-chain dehydrogenase/reductase of Thermus thermophilus HB8: a hyperthermostable aldose-1-dehydrogenase with broad substrate specificity. Chem Biol Interact. 2009 Mar 16;178(1-3):117-26

[6]Matsumoto K, Endo S, Ishikura S, Matsunaga T, Tajima K, El-Kabbani O, Hara A. Enzymatic properties of a member (AKR1C20) of the aldo-keto reductase family. Biol Pharm Bull. 2006 Mar;29(3):539-42

[7]Ishikura S, Matsumoto K, Sanai M, Horie K, Matsunaga T, Tajima K, El-Kabbani O, Hara A. Molecular cloning of a novel type of rat cytoplasmic 17beta-hydroxysteroid dehydrogenase distinct from the type 5 isozyme. J Biochem. 2006 Jun;139(6):1053-63

[8]de Oliveira JM, Simões MJ, Mora OA, Simões RS, Oliveira-Filho RM, Oliveira PB, Baracat EC, Soares JM Jr. Effects of hexestrol on mouse ovarian morphology and ovulation. Maturitas. 2008 Jun 20;60(2):153-7