17β-hydroxy Exemestane

CAT: 0931-MF-0036894Size: 1 mgDry Ice: NoHazardous: No
CAT#:0931-MF-0036894Size:1 mg
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CAS Number
122370-91-6
Target
Estrogen Receptor/ERR|||LDLR|||Androgen Receptor|||Others
Related Pathways
Others|||Endocrinology/Hormones|||Metabolism
Bioactivity
17?-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. 17?-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 ? (ER?; IC50 = 21.2 ?M) . It stimulates growth of AR- and ER?-positive MCF-7 (EC50 = 2.7 ?M) 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. 17?-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.
Smiles
C[C@@]12[C@@]3([C@]([C@]4([C@](C)(CC3)[C@@H](O)CC4)[H])(CC(=C)C1=CC(=O)C=C2)[H])[H]
Molecular Formula
C20H26O2
Molecular Weight
298.42
Shipping Conditions
Cool pack
Storage Temperature
-20°C

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