Tezacaftor-d4 (VX-661-d4) is the deuterium-labeled Tezacaftor (HY-15448), a F508del CFTR corrector. Tezacaftor helps CFTR protein reach the cell surface.
性状
Solid
体外研究(In Vitro)
氢、碳和其他元素的稳定重同位素已被掺入药物分子中,主要用作药物开发过程中定量的示踪剂。氘代因其可能影响药物的药代动力学和代谢特征而受到关注。然而,Ivacaftor (VX-770,HY-13017) 这种 CFTR 增效剂,有助于延长细胞表面 CFTR 蛋白通道的开放时间。Tezacaftor 与 Ivacaftor 结合,显示出对囊性纤维化和 CFTR Phe508del 突变纯合子疾病的有力效果。此外,Elexacaftor (VX-445,HY-111772) 也是一种 CFTR 校正器。 Elexacaftor-Tezacaftor-Ivacaftor 针对至少有一个 Phe508del 突变的囊性纤维化(CF),通常可避免肺移植适应症。 has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Treatment with VX-661 and Ivacaftor in a Phase 2 Study Resulted in Statistically Significant Improvements in Lung Function in People with Cystic Fibrosis Who Have Two Copies of the F508del Mutation. April 18, 2013