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17β-hydroxy Exemestane Sale

(Synonyms: 亚甲基宝丹酮) 目录号 : GC41300

An active metabolite of exemestane

17β-hydroxy Exemestane Chemical Structure

Cas No.:122370-91-6

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Sample solution is provided at 25 µL, 10mM.

Description

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 (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = 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.

化学性质

Cas No. 122370-91-6 SDF
别名 亚甲基宝丹酮
Canonical SMILES C=C1C2=CC(C=C[C@]2(C)[C@]3([H])[C@@]([C@@](CC[C@@H]4O)([H])[C@]4(C)CC3)([H])C1)=O
分子式 C20H26O2 分子量 298.4
溶解度 Chloroform: slightly, heated,Methanol: slightly, heated 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 3.3512 mL 16.756 mL 33.5121 mL
5 mM 0.6702 mL 3.3512 mL 6.7024 mL
10 mM 0.3351 mL 1.6756 mL 3.3512 mL
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