
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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25MG | 1521 | Get Quote |
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50MG | 2061 | Get Quote |
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Biological Information
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Product NameWAY-204688
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NoteResearch use only, not for human use.
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Brief DescriptionWAY-204688 is a selective and orally active estrogen receptor inhibitor of NF-κB transcriptional activity (IC50 = 122 nM in HAECT-1 cells).
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DescriptionWAY-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 .
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In VitroWAY-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.
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In VivoWAY-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.
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SynonymsSIM-688 | SIM688
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PathwayEndocrinology/Hormones
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TargetEstrogen Receptor/ERR
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RecptorFungal
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Research Area——
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Indication——
Chemical Information
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CAS Number796854-35-8
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Formula Weight556.62
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Molecular FormulaC34H31F3N2O2
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 100 mg/mL (179.66 mM)
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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
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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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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