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  3. WAY-204688

WAY-204688 (Synonyms: SIM-688)

Cat. No.: HY-19498
Handling Instructions

WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC50 of 122 ± 30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells.

For research use only. We do not sell to patients.

WAY-204688 Chemical Structure

WAY-204688 Chemical Structure

CAS No. : 796854-35-8

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Description

WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC50 of 122 ± 30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells.

IC50 & Target[1]

NF-κB

122 nM (IC50)

In Vitro

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[1].

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[1].

Molecular Weight

556.62

Formula

C₃₄H₃₁F₃N₂O₂

CAS No.

796854-35-8

SMILES

COC1=C([[email protected]](C2=CC=CC3=C2C=CC=C3)[[email protected]@](C)(C#N)C(N4CCC(C5=CC(C(F)(F)F)=CC=C5)CC4)=O)C=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
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Keywords:

WAY-204688SIM-688WAY204688WAY 204688SIM688SIM 688NF-κBNuclear factor-κBNuclear factor-kappaBInhibitorinhibitorinhibit

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WAY-204688
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HY-19498
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