伏环孢素

钙调磷酸酶抑制剂生物活性靶点体外研究体内研究伏环孢素试剂级价格

伏环孢素

CAS号:515814-01-4
英文名:Voclosporin
中文名:伏环孢素
CBNumber:CB42496083
分子式:C63H111N11O12
分子量:1214.65
MOL File:515814-01-4.mol

伏环孢素化学性质

沸点 :1303.8±65.0 °C(Predicted)
密度 :1.016±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :Benzene (Slightly), Methanol (Slightly)
酸度系数(pKa) :13.32±0.70(Predicted)
形态 :Solid
颜色 :White to Off-White

伏环孢素性质、用途与生产工艺

钙调磷酸酶抑制剂伏环孢素（Voclosporin）是一种新型的钙调磷酸酶抑制剂，结构上是环孢菌素A的一种类似物，修饰后活性提高3-4倍，而且具有双重、协同作用机制，通过抑制钙调磷酸酶，可阻断IL-2的表达和T细胞介导的免疫反应、稳定肾脏足细胞。与环孢素相比，伏环孢素还具有对胆固醇和甘油三酯的影响更小，糖尿病风险更低的优势。2021年2月，伏环孢素被FDA批准用于活动期、狼疮性肾炎成人患者的联合免疫抑制治疗方案。
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).