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首页 / 抑制剂/激动剂 / 膜转运蛋白 / CFTR / Ivacaftor

依伐卡托 /Ivacaftor {[allProObj[0].p_purity_real_show]}

货号：A286566 同义名： 依伐卡托 (VX-770) / VX-770

Ivacaftor is a potentiator of CFTR targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM, respectively.

Ivacaftor 化学结构 CAS号：873054-44-5
Ivacaftor 化学结构
CAS号：873054-44-5
Ivacaftor 3D分子结构
CAS号：873054-44-5
Ivacaftor 化学结构 CAS号：873054-44-5
Ivacaftor 3D分子结构 CAS号：873054-44-5
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Ivacaftor 纯度/质量文件 产品仅供科研

货号：A286566 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 CFTR ↓ 其他靶点 纯度
Ataluren ✔ 98%
Lumacaftor ++++

F508del-CFTR, EC50: 0.1 μM

 		98%
CFTR(inh)-172 +++

CFTR, Ki: 300 nM

 		99%+
GlyH-101 +

CFTR, Ki: 4.3 μM

 		99%+
IOWH-032 ++

CFTR, IC50: 1.01 μM

 		99%+
Tezacaftor ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Ivacaftor 生物活性

描述 Cystic fibrosis transmembrane conductance regulator (CFTR) is a protein kinase A-activated epithelial anion channel that is responsible for salt and fluid transport in multiple organs. Ivacaftor is a potent potentiator of CFTR. It increases forskolin-stimulated CFTR-mediated transepithelial current (IT) with an EC50 of 100 ± 47 nM in G551D-FRT cells. Also in F508del-FRT cells, ivacaftor increased forskolin-stimulated IT with an EC50 of 25 ± 5 nM. In recombinant cells expressing G551D-, F508del-, or wild-type (WT)-CFTR, 10 μM ivacaftor increased their CFTR channel open probability by ~6-fold, ~5-fold and ~2-fold, respectively. Treatment of ivacaftor significantly increased the forskolin-stimulated IT in F508del human bronchial epithelia (HBE) cells with an EC50 of 22 ± 10 nM. G551D/F508del HBE cells treated with 10μM ivacaftor for 5 days showed significant increased cilia beat frequency compared with vehicle-treated controls[1]. In the analysis of ATP-independent activity for WT-CFTR, 200 nM ivacaftor increased the activity by 2-fold, as determined by the ratio of post washout ATP-independent current to the robust ATP-induced current[2]. The bilayer studies of WT-CFTR showed that the open probability of CFTR channel treated with both 1 mM Mg-ATP and 2 μM ivacaftor was approximately twice that measured in the presence of Mg-ATP alone. The treatment of 10 μM ivacaftor on liposomes containing phosphorylated F508del-CFTR or phosphorylated G551D-CFTR increased iodide-mediated flux in the presence of 1 mM Mg-ATP[3].
作用机制 Ivacaftor potentiates CFTR function by increasing the open time of WT-CFTR, stabilizing a post-hydrolytic open state, thereby promoting decoupling between the gating cycle and ATP hydrolysis cycle[2].

Ivacaftor 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
CFBE41o- 10 µM Function Assay induces robust increases in anion transport 22768130
HBE 10 μM Function Assay 10 min augments CFTR-dependent ion transport  24106801
HBE 10 µM Function Assay augments CFTR-dependent anion transport activity 22768130
HBE 10 µM Function Assay 24 h induces a modest but significant increase in ASL depth 22768130

Ivacaftor 动物研究

Dose Rat: 10 mg/kg - 50 mg/kg[4] (p.o.) Dog: 60 mg/kg[4] (p.o.)
Administration p.o.

Ivacaftor 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03525548 Cystic Fibrosis Phase 3 Active, not recruiting March 2019 -
NCT03447249 Cystic Fibrosis Phase 3 Active, not recruiting April 16, 2019 -
NCT03525574 Cystic Fibrosis Phase 3 Enrolling by invitation June 2021 -

Ivacaftor 参考文献

[1]Van Goor F, Hadida S, et al. Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770. Proc Natl Acad Sci U S A. 2009;106(44):18825-30.

[2]Jih KY, Hwang TC. Vx-770 potentiates CFTR function by promoting decoupling between the gating cycle and ATP hydrolysis cycle. Proc Natl Acad Sci U S A. 2013;110(11):4404-9.

[3]Eckford PD, Li C, et al. Cystic fibrosis transmembrane conductance regulator (CFTR) potentiator VX-770 (ivacaftor) opens the defective channel gate of mutant CFTR in a phosphorylation-dependent but ATP-independent manner. J Biol Chem. 2012;287(44):36639-49.

Ivacaftor 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.25mL

12.74mL

2.55mL

1.27mL

25.48mL

5.10mL

2.55mL

Ivacaftor 技术信息

CAS号873054-44-5
分子式C24H28N2O3
分子量 392.491
别名 依伐卡托 (VX-770) ;VX-770
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 50 mg/mL(127.39 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 4 mg/mL clear

PO 0.5% CMC-Na 38 mg/mL suspension

Tags: Ivacaftor | 873054-44-5 | VX-770 | VX770 | VX 770 | Membrane Transporter/Ion Channel | Autophagy | CFTR | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Ivacaftor 纯度/质量文件 | Ivacaftor 亚型比较 | Ivacaftor 生物活性 | Ivacaftor 细胞研究 | Ivacaftor 动物研究 | Ivacaftor 临床数据 | Ivacaftor 参考文献 | Ivacaftor 实验方案 | Ivacaftor 技术信息

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