Prinaberel

CAS No. 524684-52-4

Prinaberel( —— )

Catalog No. M37942 CAS No. 524684-52-4

Prinaberel (ERB-041) is an effective and selective ERβ agonist and >200-fold selective for ERβ.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Prinaberel
  • Note
    Research use only, not for human use.
  • Brief Description
    Prinaberel (ERB-041) is an effective and selective ERβ agonist and >200-fold selective for ERβ.
  • Description
    Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis.
  • In Vitro
    Prinaberel (ERB-041) (0-60 μM; 24 hours) treatment of human SCC cells induces cell differentiation, cell cycle arrest and reduces colony formation.Prinaberel shows a marked reduction in the expression of inflammation regulatory proteins such as p-NFκBp65, iNOS and COX-2 in A431 cells. Prinaberel diminishes phosphorylated-PI3K and -AKT, which is associated with the enhancement in E-cadherin expression and reduction in migration of A431 cells.Prinaberel (0.01-10 μM) inhibits cell proliferation in a dose- and time-dependent manner.Prinaberel (10 μM; 48 hours) promotes ovarian cancer (SKOV-3 cells) apoptosis.Western Blot Analysis Cell Line:A431 cells Concentration:0, 20, 40 and 60 μM Incubation Time:24 hours Result: Reduction in the expression of G1 cyclins (D1, D2 and D3) and CDK4.Cell Proliferation Assay Cell Line:SKOV-3, A2780CP or OVCAR-3 cells Concentration: 0.01, 0.1 and 10 μM Incubation Time:24-48 hours Result:Showed significantly inhibitory effect on cell proliferation.
  • In Vivo
    Prinaberel (2mg/mouse; topically; 30 min prior to UVB irradiation for 30 weeks) suppresses development of squamous cell carcinoma in SKH-1 hairless mice.Prinaberel reduces proliferation and angiogenesis and induces apoptosis in UVB-induced skin tumors. Prinaberel suppresses pro-inflammatory signaling pathway in UVB-induced skin tumors. Prinaberel diminished tumor invasiveness via PI3K-AKT pathway and WNT signaling.Animal Model:Six- to eight-weeks-old SKH-1 hairless female mice Dosage:2 mg/mouse in 200μl ethanol Administration:Topically; 30 min prior to UVB (180mJ/cm2) irradiation for 30 weeksResult:Diminished UVB-induced skin tumor development in SKH-1 hairless mice.
  • Synonyms
    ——
  • Pathway
    Endocrinology/Hormones
  • Target
    Estrogen Receptor/ERR
  • Recptor
    Estrogen/progestogen Receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    524684-52-4
  • Formula Weight
    271.24
  • Molecular Formula
    C15H10FNO3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : ≥ 40 mg/mL (147.47 mM)
  • SMILES
    Oc1cc(C=C)c2oc(nc2c1)-c1ccc(O)c(F)c1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Malamas MS, et al. Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands. J Med Chem. 2004;47(21):5021-5040.?
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