PHTPP 是选择性的雌激素受体 β 拮抗剂，其选择性比 ERα 高 36 倍。

PHTPP is a selective ERβ antagonist.

PHTPP is a selective ERβ antagonist. PHTPP reduces FSH-mediated cAMP production by 80% (p<0.01) while it has no effect on basal cAMP. PHTPP (10-6 M) inhibits E2-stimulated ERβ activity. However, it does not suppress E2-stimulated ERα activity. A high dose of PHTPP (10-6 M) slightly increases class 1 Igf1 mRNA expression, and facilitates the DPN-induced increase in class 1 Igf1 mRNA expression.

Cells are plated at a density of 3 to 4×10^5 in 1 mL of medium per well in a 24-well plate for cell viability and cAMP analysis. Cells are cultured in Dulbecco's Modified Eagle Medium with PHTPP (1 μM), or ethanol (0.1%) as the vehicle. The incubator is set to an atmosphere of 5% CO2 in air at 37°C, and cultures are allowed to acclimate for at least 24 h. The culture medium is then aspirated and replaced with serum-free DMEM/F12 containing 0.1 μM androstenedione. The cells are collected for intracellular cAMP and to test cell viability. They are for reference only.

805239-56-9

C20H11F6N3O

423.318

DMSO:14 mg/mL(33 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years