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WAY-204688(SIM-688)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
WAY-204688(SIM-688)图片
CAS NO:796854-35-8
规格:98%
分子量:556.62
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
WAY-204688是雌激素受体(ER-α)选择性的,口服活性的NF-κB转录活性抑制剂。在HAECT细胞中,作用于NF-κB-Luc荧光素酶,IC50为122 ± 30nM。
CAS:796854-35-8
分子式:C34H31F3N2O2
分子量:556.62
纯度:98%
存储:Store at -20°C

Background:

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.


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[1].


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].


[1]. Caggiano TJ, et al. Estrogen receptor dependent inhibitors of NF-kappaB transcriptional activation-1 synthesis and biological evaluation of substituted 2-cyanopropanoic acid derivatives: pathway selective inhibitors of NF-kappaB, a potential treatment for rheumatoid arthritis. J Med Chem. 2007 Nov 1;50(22):5245-8.