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Peficitinib
Peficitinib

基本信息 产品名称 Peficitinib
英文名称 4-[[(1R,3S)-5-hydroxy-2-adamantyl]amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide  
别名 ASP015K; JNJ-54781532; ASP-015K; ASP 015K; JNJ54781532; JNJ 54781532  
CAS 944118-01-8  
分子式 C18H22N4O2  
分子量 326.39  

物化性质 bp
nD20  
density  
fp  
外观 淡黄色固体  

运输信息
UNNumber  
Class  
PG  
危险性描述  
安全性描述  

用途信息
用途 Peficitinib (ASP015K,JNJ-54781532) 是一种新型口服的Janus激酶 (JAK) 抑制剂, Peficitinib抑制JAK1, JAK2, JAK3和TYK2酶活性, IC50分别为3.9, 5.0, 0.71, 和4.8 nM。  

其它信息 Peficitinb (ASP015K, JNJ-54781532) is a novel oral Janus kinase (JAK) inhibitor. Peficitinib inhibits JAK1, JAK2, JAK3 and Tyk2 enzyme activities with IC50s of 3.9, 5.0, 0.71 and 4.8 nM, respectively, and has moderate selectivity for JAK3 inhibition.
IC50 value: 3.9/5.0/0.71 nM (for JAK1/2/3) , 4.8 nM (for Tyk2)
Target: JAK
Peficitinib (ASP015K) is a novel orally bioavailable JAK inhibitor in development for the treatment of severe rheumatoid arthritis (RA). Milder inhibition of JAK2 by Peficitinib may contribute to the mitigation of effects on red blood cells and platelets reported to be caused by JAK2 inhibition. Moreover, Peficitinib has shown an improvement in symptoms in RA animal models after once-daily oral administration, and has demonstrated dose-dependent improvement in psoriatic disease activities in a 6-week phase IIa study. The terminal mean half-life of Peficitinib was estimated to be 7-13 h in pharmacological studies with healthy subjects, suggesting that Peficitinib can be dosed once-daily in the next development stage.


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