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Hexestrol

产品号 S2473 公司名称 Selleck Chemicals
CAS号 84-16-2 公司网站 http://www.selleckchem.com
分子式 C18H22O2 电 话 (877) 796-6397
分子量 270.36608 传 真 (832) 582-8590
纯 度 电子邮件 sales@selleckchem.com
保 存 -20°C Chembase数据库ID: 5561

产品价格信息

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产品别名

标题
Hexestrol
IUPAC标准名
4-[(3R,4S)-4-(4-hydroxyphenyl)hexan-3-yl]phenol
IUPAC传统名
hexestrol
别名
Bibenzyl
Dihydro-stilbestro
Cycloestrol

产品登记号

CAS号 84-16-2

产品性质

作用靶点 Estrogen receptor
成盐信息 Free Base
保存条件 -20°C

产品详细信息

详细说明 (English)
Research Area
Description Cancer
Biological Activity
Description Hexestrol binds to Erα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively.
Targets ERα ERβ
IC50 0.07 nM (EC50) 0.175 nM (EC50) [1]
In Vitro Hexestrol binds to ERα with EC50 of 0.07 nM and to ERβ with EC50 of 0.175 nM. [1] Hexestrol inhibits activity of AKR1B13 with IC50 of 3.2 μM. [2] Hexestrol inhibits the d-galactose dehydrogenase activity of thermophilus aldose 1-dehydrogenase with IC50 of 0.063 mM. [3] Hexestrol inhibits the dehydrogenase activity of AKR1C20 towards 10 μM 4-androsten-3α-o1-17-one with IC50 values of 2.7 μM. [4] Hexestrol inhibits 17HSD5 with IC50 of 30 μM, and inhibits TBER1 with IC50 of 0.8 μM. [5] Hexestrol reacts with DNA through the catechol quinone, thus can be a carcinogen. [6]
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. [7]
Clinical Trials
Features Much higher ERβ binding selectivity than Erα
Protocol
Kinase Assay [1]
Estrogen Receptor Binding Affinity Assays Relative binding affinities are determined by a competitive radiometric binding assay, using 10 nM [3H]estradiol as tracer, and purified full-length human ERα and ERβ. Incubations are for 18–24 h at 0 °C, then the receptor-ligand complexes are absorbed onto hydroxyapatite and unbound ligand is washed away. The binding affinities are expressed as relative binding affinity (RBA) values, with the RBA of estradiol set to 100. The values given are the average ± range or SD of two or more independent determinations. Hexestrol is tested as racemate.
Animal Study [7]
Animal Models adult mice aged 90-120 days
Formulation Saline
Doses 3 mg/kg and 6 mg/kg
Administration administered intraperitoneally once daily for 30 days
References
[1] Waibel M, et al. Eur J Med Chem, 2009, 44(9), 3412-3424.
[2] Endo S, et al. Chem Biol Interact, 2009, 178(1-3), 151-157.
[3] Asada Y, et al. Chem Biol Interact. 2009, 178(1-3), 117-126.
[4] Matsumoto K, et al. Biol Pharm Bull, 2006, 29(3), 539-542.
[5] Ishikura S, et al. J Biochem, 2006, 139(6), 1053-1063.
[6] Ishikura S, et al. Ann N Y Acad Sci, 2004, 1028, 247-257.