17β-hydroxy Exemestane (Synonyms:亚甲基宝丹酮;17-β-羟基依西美坦;四氧化二铁铜;乙烯基环丙烷;17Β-羟基依西美坦)
目录号 : KCM10729 CAS No. : 122370-91-6 纯度 : ≥98%
17β-hydroxy Exemestane is the primary active metabolite of exemestane . It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11. 17β-hydroxy Exemestane is an aromatase inhibitor (IC = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC = 2.7 μM) and T47D breast cancer cells (ECs = 0.43 and 1,500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7aro cells in a concentration-dependent manner. 17β-hydroxy Exemestane (20 mg/kg) inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae, in ovariectomized rats.
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1mg
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5mg
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生物活性

17β-Hydroxy exemestane (17-H-EXE) is the primary active metabolite of Exemestane. 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats.

分子式
C20H26O2
分子量
298.41924
CAS号
122370-91-6
中文名称
亚甲基宝丹酮
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
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