| Identification | Back Directory | [Name]
WAY-204688 | [CAS]
796854-35-8 | [Synonyms]
SIM-688
WAY-204688
1-Piperidinepropanenitrile, α-[(S)-(2-methoxyphenyl)-1-naphthalenylmethyl]-α-methyl-β-oxo-4-[3-(trifluoromethyl)phenyl]-, (αS)- | [Molecular Formula]
C34H31F3N2O2 | [MDL Number]
MFCD30532597 | [MOL File]
796854-35-8.mol | [Molecular Weight]
556.63 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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