515814-01-4
515814-01-4 結構式
基本信息
狼瘡腎炎
伏環(huán)孢素
揮發(fā)性孢子蛋白
化合物 T17235
伏環(huán)孢素VOCLOSPORIN
R 1524
Luveniq
Isatx247
Isatx-247
Isatx 247
Voclosporin
Voclosporine
Voclosporin [usan]
Voclosporin USP/EP/BP
物理化學性質
常見問題列表
Calcineurin
This novel semi-synthetic calcineurin (CN) inhibitor is designated Voclosporin (ISATX247). The efficacy of Voclosporin as an immunosuppressive agent is examined using an in vitro calcineurin assay. Voclosporin (ISATX247) is a calcineurin inhibitor that has shown more potency than Cyclosporine in vitro.
伏環(huán)孢素合成起始于較高級的中間體環(huán)孢素A 14.1，這是一種能夠通過發(fā)酵法獲得的天然產(chǎn)物。將環(huán)孢素A
14.1與乙酸酐、吡啶和DMAP在二氯甲烷中處理，得到了收率良好的乙?；h(huán)孢素A
14.2。中間體14.2接著經(jīng)過臭氧裂解反應，生成了氧化加成產(chǎn)物14.3。在銀高氯酸鹽存在下，使用丙炔三甲基硅烷和雙(環(huán)戊二烯基)鋯氯化氫對醛14.3進行同系化反應（Homologation
Reactions），得到了反式烯烴14.4。最后，通過堿介導的乙?；コ磻闪薞oclosporin（14），隨后通過半制備高壓液相色譜（HPLC）進行純化。
All animals tolerate Voclosporin (ISATX247) and Cyclosporine A (CsA) very well. There are no severe adverse effects associated with either drug. In the Voclosporin group, all animals except 1 have diarrhea of different durations during the study (mean 2.3 days, range 2 to 7 days). This differs from the CsA and the control groups, where no animals have diarrhea. Mean weight loss at the end of the study is slightly higher in the Voclosporin group than in the CsA and control groups (3.4% vs 2.0% and 1.0%, respectively).