WAY-204688
- Product Name
- WAY-204688
- CAS No.
- 796854-35-8
- Chemical Name
- WAY-204688
- Synonyms
- SIM-688;WAY-204688;(2S,3S)-3-(2-Methoxyphenyl)-2-methyl-3-(naphthalen-1-yl)-2-(4-(3-(trifluoromethyl)phenyl)piperidine-1-carbonyl)propanenitrile;1-Piperidinepropanenitrile, α-[(S)-(2-methoxyphenyl)-1-naphthalenylmethyl]-α-methyl-β-oxo-4-[3-(trifluoromethyl)phenyl]-, (αS)-
- CBNumber
- CB53175601
- Molecular Formula
- C34H31F3N2O2
- Formula Weight
- 556.63
- MOL File
- 796854-35-8.mol
WAY-204688 Property
- Boiling point:
- 708.7±60.0 °C(Predicted)
- Density
- 1.231±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Solid
- pka
- -1.66±0.40(Predicted)
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- CS-6666
- Product name
- WAY-204688
- Purity
- 99.89%
- Packaging
- 1mg
- Price
- $480
- Updated
- 2021/12/16
WAY-204688 Chemical Properties,Usage,Production
Uses
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.
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].
IC 50
NF-κB-luc: 122 nM (IC50, in HAECT-1 cell); NF-κB
References
[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. DOI:10.1021/jm701013k
WAY-204688 Preparation Products And Raw materials
Raw materials
Preparation Products
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