WAY-204688

CAS No. 796854-35-8

WAY-204688( SIM-688 | SIM688 )

Catalog No. M26862 CAS No. 796854-35-8

WAY-204688 is a selective and orally active estrogen receptor inhibitor of NF-κB transcriptional activity (IC50 = 122 nM in HAECT-1 cells).

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    WAY-204688
  • Note
    Research use only, not for human use.
  • Brief Description
    WAY-204688 is a selective and orally active estrogen receptor inhibitor of NF-κB transcriptional activity (IC50 = 122 nM in HAECT-1 cells).
  • Description
    WAY-204688 is a selective and orally active estrogen receptor inhibitor of NF-κB transcriptional activity (IC50 = 122 nM in HAECT-1 cells).(In Vitro):WAY-204688 displaces [3H]E2 from the ERα ligand-binding domain protein (C50=2.43 μM) and from the ERβ ligand-binding domain protein (IC50=1.5 μM).(In Vivo):WAY-204688 (5 mg/kg per day, p.o.) inhibits pro-inflammatory genes including MHI, VCAM-1, RANTES, and TNF-α and induces the gene products and uterine wet weight. WAY-204688 (0.3 mg/kg, p.o.) is active in the Lewis rat adjuvant-induced arthritis model .
  • In Vitro
    WAY-204688 is ER-dependenrt (activity seen only when hER is coexpressed with NF-κB-luciferase in human aortic endothelial cell lines (HAECT-1) cells). The interaction of WAY-204688 with ERα and ERβ is examined in vitro. WAY-204688 displaces [3H]E2 from the ERα ligand binding domain protein (LBD) with IC50=2.43 μM and from the ERβ ligand binding domain protein(LBD) with IC50=1.5 μM.
  • In Vivo
    WAY-204688 (5 mg/kg per day, po daily for 5 weeks) is evaluated in vivo for the ability to inhibit four proinflammatory genes (MHC, invariant chain (MHI), VCAM-1, RANTES, and TNF-α). The effect of WAY-204688 on induction of the gene products and on uterine wet weight is compared to that of 17α-ethinyl 17β-estradiol (EE at 10 μg/kg per day) in the same paradigm. Further characterization of WAY-204688 is carried out in several preclinical models of inflammatory disease. In the Lewis rat adjuvant-induced arthritis model (AIA), WAY-204688 is active at a dose of 0.3 mg/kg per day, po.
  • Synonyms
    SIM-688 | SIM688
  • Pathway
    Endocrinology/Hormones
  • Target
    Estrogen Receptor/ERR
  • Recptor
    Fungal
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    796854-35-8
  • Formula Weight
    556.62
  • Molecular Formula
    C34H31F3N2O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (179.66 mM)
  • SMILES
    [C@H]([C@](C(=O)N1CCC(CC1)C2=CC(C(F)(F)F)=CC=C2)(C#N)C)(C=3C4=C(C=CC3)C=CC=C4)C5=C(OC)C=CC=C5
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.Hajime Iwamura, et al. Antifungal Activity of Substituted 7-(β-D-Ribofuranosyl)pyrrolo-[2,3-d]pyrimidines. Agricultural and Biological Chemistry, Volume 40, Issue 7, 1 July 1976, Pages
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