805239-56-9

805239-56-9 structure

Name: PHTPP
Chemical Name: 4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol
CAS Number: 805239-56-9
Molecular Formula: C₂₀H₁₁F₆N₃O
Molecular Weight: 423.31100
Catalog: Research Areas Cancer
Create Date: 2016-03-27 00:05:00
Modify Date: 2024-01-09 11:21:28
PHTPP is a selective ERβ antagonist.

Name	4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol
Synonyms	hms3269l05 phtpp

Description	PHTPP is a selective ERβ antagonist.
Related Catalog	Signaling Pathways >> Others >> Estrogen Receptor/ERR Research Areas >> Cancer
Target	ERβ[1]
In Vitro	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[1]. PHTPP (10-6 M) inhibits E2-stimulated ERβ activity, but 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[2].
Cell Assay	Cells are plated at a density of 3 to 4×105 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[1].
References	[1]. Compton DR, et al. Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor beta antagonist activity. J Med Chem. 2004 Nov 18;47(24):5872-93.