中文名称:

Voclosporin

中文同义词:

英文名称:

Voclosporin

英文同义词:

Isatx 247;Isatx247;Isatx-247;Luveniq;Lx211;R 1524;Voclosporin;Voclosporin [usan]

CAS号:

515814-01-4

分子式:

C63H111N11O12

分子量:

1214.65

EINECS号:

相关类别:

多肽抑制剂;Intermediates Fine Chemicals;Peptides;Pharmaceuticals

Mol文件:

515814-01-4.mol

沸点 

1303.8±65.0 °C(Predicted)

密度 

1.016±0.06 g/cm3(Predicted)

酸度系数(pKa)

13.32±0.70(Predicted)

生物活性

Voclosporin (ISAtx-247) 是一种钙调神经磷酸酶 (CN; PP2B) 抑制剂。

靶点

Calcineurin

体外研究

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.

体内研究

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).