PHTPP

SKU: orb1302898

Description

PHTPP is a potent and selective antagonist of the estrogen receptor beta (ERβ). It is a valuable research tool for investigating ERβ-specific signaling in cellular assays and animal models, particularly in studies of endocrinology, oncology, and neuroscience.

Research Area

Metabolism Research

Key Properties

• CAS Number: 805239-56-9
• MW: 423.31
• Purity: 99.72% (May vary between batches)
• Formula: C₂₀H₁₁F₆N₃O
• SMILES: Oc1ccc(cc1)-c1c(nn2c(cc(nc12)C(F)(F)F)C(F)(F)F)-c1ccccc1
• Target: Estrogen/progestogen Receptor,Estrogen Receptor/ERR
• Solubility: H2O:< 1 mg/mL (insoluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.72 mM);DMSO:22.73 mg/mL (53.7 mM);Ethanol:3.96 mg/mL (9.35 mM)

Bioactivity

• In Vitro:
  PHTPP acts as a selective antagonist for estrogen receptor beta (ERβ), significantly decreasing follicle-stimulating hormone (FSH)-mediated cyclic AMP (cAMP) production by 80% (p<0.01), without impacting basal cAMP levels. At a concentration of 10^-6 M, PHTPP inhibits estradiol (E2)-stimulated ERβ activity but does not affect E2-induced ERα activity. Furthermore, a high concentration of PHTPP (10^-6 M) marginally enhances class 1 Igf1 mRNA expression and promotes the DPN-induced increase in class 1 Igf1 mRNA expression.
• Cell Research:
  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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

progestogenReceptor, progestogen Receptor, PHTPP, inhibit, Inhibitor, ERβ, ERR, Estrogen Receptor, EstrogenReceptor, Estrogen Receptor/ERR

Compound Identifiers

PubChem CID

11201035