WAY-204688

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

WAY-204688 是一种选择性、口服活性雌激素受体 NF-κB 转录活性抑制剂（在 HAECT-1 细胞中 IC50 = 122 nM）。

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 .

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.

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.

SIM-688 | SIM688

Endocrinology/Hormones

Estrogen Receptor/ERR

Fungal

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796854-35-8

556.62

C34H31F3N2O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (179.66 mM)

[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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(-20℃)

With Ice Pack

≥ 2 years