Ivacaftor (VX-770)

别名: VX-770 中文名称:依伐卡托

Ivacaftor (VX-770)是一种CFTR的选择性增强剂,靶向作用于G551D-CFTRF508del-CFTR,在fisher大鼠甲状腺细胞中EC50分别为100 nM和25 nM。

Ivacaftor (VX-770) Chemical Structure

Ivacaftor (VX-770) Chemical Structure

CAS: 873054-44-5

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 919.69 现货
5mg RMB 1374.83 现货
50mg RMB 7957.63 现货
200mg RMB 11384.1 现货
1g RMB 16134.3 现货
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客户使用Selleck的Ivacaftor (VX-770)发表文献229

产品质控

批次: 纯度: 99.97%
99.92

常与Ivacaftor (VX-770)一起在实验中被使用的化合物

Tezacaftor (VX-661)


Tezacaftor专门针对F508del CFTR,而Ivacaftor同时针对G551D-CFTR和F508del-CFTR。

Elexacaftor (VX-445)


Elexacaftor在增强III类和IV类CFTR突变方面与Ivacaftor表现出倍增协同作用。

Shaughnessy CA, et al. Scientific reports 11.1 (2021): 19810.

Lumacaftor (VX-809)


Ivacaftor和Lumacaftor用于治疗F508del突变纯合个体的囊性纤维化。

Cheng PC, et al. Expert Rev Respir Med. 2019 May; 13(5): 417–423.

CFTRinh-172


Ivacaftor(VX-770)是一种CFTR增强剂,而CFTRinh-172是一种CFTR抑制剂。

Laselva O, et al. Eur Respir J. 2021 Jun; 57(6): 2002774.

Icenticaftor (QBW251)


Ivacaftor和Icenticaftor是CFTR的小分子通道增强剂,其在慢性阻塞性肺疾病中的作用正在进行临床试验。

Dransfield M, et al. American journal of respiratory and critical care medicine 205.6 (2022): 631-640.

Ivacaftor (VX-770)相关产品

相关信号通路图

CFTR抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
HBE  Function Assay 10 µM 24 h induces a modest but significant increase in ASL depth 22768130
HBE  Function Assay 10 μM 10 min augments CFTR-dependent ion transport  24106801
HBE  Function Assay 10 µM augments CFTR-dependent anion transport activity 22768130
CFBE41o- Function Assay 10 µM induces robust increases in anion transport 22768130
HBE  Function Assay 10 µM potentiates CFTR-dependent Isc, regardless of prior administration of CSE 22768130
HBE  Function Assay 10 µM partially restores depletion of ASL depth in CSE treated monolayers 22768130
mouse NIH-3T3 cells Function assay 30 mins Potentiation of human CFTR F508del mutant expressed in mouse NIH-3T3 cells after 30 mins by fluorescent voltage sensing optical assay, EC50 = 0.003 μM. 25441013
human CFBE41o cells Function assay 10 mins Potentiation of CFTR F508del mutant (unknown origin) expressed in human CFBE41o cells incubated for 10 mins in presence of forskolin measured for 7 secs by YFP halide assay, EC50 = 0.126 μM. 29148763
HEK293 cells Function assay 10 mins Potentiation of CFTR G551D mutant (unknown origin) expressed in HEK293 cells incubated for 10 mins in presence of forskolin measured for 2 mins by YFP halide assay, EC50 = 1.3 μM. 29148763
human bronchial epithelial cells Function assay Potentiation of human CFTR F508del/G551D mutant in human bronchial epithelial cells by Ussing chambers recording technique, EC50 = 0.022 μM. 25441013
human bronchial epithelial cells Function assay Potentiation of human CFTR F508del mutant in human bronchial epithelial cells by Ussing chambers recording technique, EC50 = 0.236 μM. 25441013
NRK-49F cells Function assay Inhibition of TGF-beta1-induced total collagen accumulation in rat NRK-49F cells, IC50 = 4 μM. 25467157
DAOY cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
NB-EBc1 cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
MG 63 (6-TG R) cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
RD cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
SK-N-MC cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
Saos-2 cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 Ivacaftor (VX-770)是一种CFTR的选择性增强剂,靶向作用于G551D-CFTRF508del-CFTR,在fisher大鼠甲状腺细胞中EC50分别为100 nM和25 nM。
靶点
F508del-CFTR [1]
(Fisher rat thyroid cells)
G551D-CFTR [1]
(Fisher rat thyroid cells)
25 nM(EC50) 100 nM(EC50)
体外研究(In Vitro)
体外研究活性

Ivacaftor(10 μM) 作用于表达CFTR突变型G551D的Fisher 大鼠甲状腺(FRT) 细胞,显著提高forskolin-刺激的Cl-分泌(IT),提高~4倍,EC50为100 nM,作用于表达CFTR突变型F508del进程的重组细胞,提高6倍,EC50为25 nM。与提高forskolin刺激的IT相一致,Ivacaftor(10 μM) 提高G551D-, F508del-, 和野生型CFTR 的开放概率(Po),分别提高~6倍,~5倍 和~2倍。说明Ivacaftor 直接作用于CFTR,而提高活性。Ivacaftor(10 μM)作用于携带G551D 和F508del CFTR 突变型的原代培养的人 CF 支气管上皮细胞(HBE),有效提高 forskolin-刺激的IT,提高10倍,从5%提高到最高水平48%,EC50为236 nM,有效性比通常使用的CFTR 增强剂Genistein高70多倍,EC50 为16 μM。Ivacaftor作用于携带F508del纯合子CFTR的HBE, 显著提高forskolin刺激的IT,EC50为22 nM, 从4%提高到16%。因为CFTR增强, Ivacaftor抑制过多ENaC-调节的Na+和液体吸收,IC50为43 nM, 且作用于G551D/F508del HBE,降低amiloride反应, 导致表面液体和纤毛摆动频率(CBF)提高。[1]

实验图片 检测方法 检测指标 实验图片 PMID
Western blot PPARγ / pERK NLRP3 Rδf508 30498130
Immunofluorescence F-actin 30498130
体内研究(In Vivo)
体内研究活性

Ivacaftor作用于携带G551D突变的,年龄6到11的囊性纤维化对象,已经完成三期研究。

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05519020 Recruiting
Cystic Fibrosis
Sheffield Teaching Hospitals NHS Foundation Trust
July 27 2022 --
NCT04254705 Withdrawn
Cystic Fibrosis
Universitaire Ziekenhuizen KU Leuven|Vertex Pharmaceuticals Incorporated|KU Leuven|University of Lisbon
March 1 2020 Not Applicable
NCT03085485 Completed
Chronic Obstructive Pulmonary Disease|Chronic Bronchitis
University of Alabama at Birmingham|National Heart Lung and Blood Institute (NHLBI)|Vertex Pharmaceuticals Incorporated
March 16 2017 Phase 2
NCT02724527 Unknown status
Cystic Fibrosis
Nivalis Therapeutics Inc.
April 2016 Phase 2

化学信息&溶解度

分子量 392.49 分子式

C24H28N2O3

CAS号 873054-44-5 SDF Download Ivacaftor (VX-770) SDF
Smiles CC(C)(C)C1=CC(=C(C=C1NC(=O)C2=CNC3=CC=CC=C3C2=O)O)C(C)(C)C
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 79 mg/mL ( 201.27 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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