CAS:1152311-62-0VX-661

Synonyms: Tezacaftor

VX-661 is a F508del CFTR corrector and is believed to help CFTR protein reach the cell surface.

规格	价格	促销价格	库存

18817579266

立即询价

咨询

18817579266

立即询价

实验数据

技术信息

CAS号

1152311-62-0

储存条件

分子式

C26H27F3N2O6

运输

蓝冰

分子量

520.50

别名

Tezacaftor

溶解度

DMSO	500.0 mg/mL (960.6 mM)
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	10 mg/mL	clear
PO	0.5% CMC-Na	52 mg/mL	suspension

生物活性

描述Cystic fibrosis is caused by a reduced quantity or function of cystic fibrosis transmembrane conductance regulator (CFTR) protein, owing to mutations in CFTR. VX-661 is a first-generation CFTR corrector that has shown enhanced CFTR function and improved lung function in a phase 2 clinical trial involving patients who were homozygous for the Phe508del mutation or heterozygous for the Phe508del and G551D mutations. The combination of VX-445 (2 μM) and VX-661 (18 μM) increased levels of mature CFTR protein and led to an increase in human bronchial epithelial cells from Phe508del–MF (a minimal-function mutation) and Phe508del–Phe508del (the Phe508del CFTR mutation) donors. All doses of [VX-659-VX-661-ivacaftor] resulted in significant improvement in the percentage of predicted FEV₁ (forced expiratory volume in 1 second) as compared with the respective within-group baseline values at day 29 in patients with Phe508del-MF or Phe508del-Phe508del genotypes.