515814-01-4
515814-01-4 结构式
基本信息
狼疮肾炎
伏环孢素
挥发性孢子蛋白
化合物 T17235
伏环孢素VOCLOSPORIN
R 1524
Luveniq
Isatx247
Isatx-247
Isatx 247
Voclosporin
Voclosporine
Voclosporin [usan]
Voclosporin USP/EP/BP
物理化学性质
常见问题列表
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.
伏环孢素合成起始于较高级的中间体环孢素A 14.1，这是一种能够通过发酵法获得的天然产物。将环孢素A
14.1与乙酸酐、吡啶和DMAP在二氯甲烷中处理，得到了收率良好的乙酰基环孢素A
14.2。中间体14.2接着经过臭氧裂解反应，生成了氧化加成产物14.3。在银高氯酸盐存在下，使用丙炔三甲基硅烷和双(环戊二烯基)锆氯化氢对醛14.3进行同系化反应（Homologation
Reactions），得到了反式烯烃14.4。最后，通过碱介导的乙酰基去除反应生成了Voclosporin（14），随后通过半制备高压液相色谱（HPLC）进行纯化。
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).