PHTPP

SKU: orb1223962

Description

A potent, selective antagonist of estrogen ERβ receptor; exhibits 36-fold selective for ERβ, and is fully effective as an ERα antagonist, while exhibiting no significant agonism on ERβ or Erα; enhances SKOV3 and OV2008 ovarian cancer cell growth in in vitro assays.

Key Properties

• CAS Number: 805239-56-9
• MW: 423.3
• Purity: >98% (HPLC)
• Formula: C₂₀H₁₁F₆N₃O
• SMILES: OC1=CC=C(C2=C3N=C(C(F)(F)F)C=C(C(F)(F)F)N3N=C2C4=CC=CC=C4)C=C1
• Target: Estrogen Receptor/ERR
• Solubility: DMSO: 14 mg/mL (33 mM) （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PHTPP

Quick Database Links

Gene Symbol

Estrogen Receptor/ERR