Ivacaftor (VX-770)

目录号:S1144 别名: VX-770 中文名称:依伐卡托

仅限科研使用

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

CAS: 873054-44-5

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 919.69 现货
RMB 1374.83 现货
RMB 7957.63 现货
RMB 11384.1 现货
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客户使用Selleck生产的Ivacaftor (VX-770)发表文献191篇:

产品安全说明书

CFTR抑制剂选择性比较

相关CFTR产品

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。
特性 The first potent and orally available CFTR potentiator to enter human clinical trials.
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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HBE  NXT4cGF1TnWwY4Tpc44hSXO|YYm= NUXpOYVDOTBizszN NH71b|YyOCCvaX6= M4Xib4F2\22nboTzJGNHXFJvZHXw[Y5l\W62IHnvckB1emGwc4DvdpTDqA>? NFfl[Y09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGwOlgxOSd-MkSxNFY5ODF:L3G+
CFBE41o- M2jHdWZ2dmO2aX;uJGF{e2G7 NYXUbnlWOTBiwsXN NGfVSYdqdmS3Y3XzJJJw[nW|dDDpcoNz\WG|ZYOgbY4h[W6rb36geJJidnOyb4L0 NUXsPXNERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3OlgyOzBpPkKyO|Y5OTNyPD;hQi=>
HBE  M3vocmZ2dmO2aX;uJGF{e2G7 NEm4OHAyOCEEtV2= NXLy[mJX[XWpbXXueJMhS0[WUj3k[ZBmdmSnboSgZY5qd25idILhcpNxd3K2IHHjeIl3cXS7 MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjd4OEGzNEc,OjJ5NkixN|A9N2F-
HBE  NWfTfHB4TnWwY4Tpc44hSXO|YYm= NVTBU|hpOTBiwsXN NYnMSm43OjRiaB?= NU\4VmM2cW6mdXPld{BiKG2xZHXzeEBjfXRic3nncolncWOjboSgbY5kemWjc3WgbY4hSVOOIHTldJRp NVLCcFZrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3OlgyOzBpPkKyO|Y5OTNyPD;hQi=>
HBE  MVvGeY5kfGmxbjDBd5NigQ>? NHjFZpIyOCEEtV2= NVnlbnVueG:2ZX70bYF1\XNiQ1\UVk1l\XCnbnTlcpQhUXOlLDDy[YdiemSuZYPzJI9nKHC{aX;yJIFldWmwaYP0doF1cW:wIH;mJGNUTQ>? NV;D[np3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3OlgyOzBpPkKyO|Y5OTNyPD;hQi=>
HBE  NGHyUIhHfW6ldHnvckBCe3OjeR?= NXTuRYFYOTBiwsXN M3LFbZBienSrYXzsfUBz\XO2b4Lld{Bl\XCuZYTpc44hd2ZiQWPMJIRmeHSqIHnuJGNUTSC2cnXheIVlKG2xbn;sZZlmenN? NVT0SZlWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3OlgyOzBpPkKyO|Y5OTNyPD;hQi=>
mouse NIH-3T3 cells MmrXSpVv[3Srb36gZZN{[Xl? M3zOZlMxKG2rboO= NV;RNJJZWG:2ZX70bYF1cW:wIH;mJIh2dWGwIFPGWHIhTjVyOHTlcEBufXSjboSg[ZhxemW|c3XkJIlvKG2xdYPlJG5KUC1|VEOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwdDD2c4x1[WenIIPlcpNqdmdib4D0bYNidCCjc4PhfUwhTUN3MDC9JFAvODB|IN88UU4> NHW1S|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS0NVAyOyd-MkW0OFExOTN:L3G+
human bronchial epithelial cells M2myOWZ2dmO2aX;uJIF{e2G7 NVn0Om9IWG:2ZX70bYF1cW:wIH;mJIh2dWGwIFPGWHIhTjVyOHTlcE9IPTVzRDDteZRidnRiaX6gbJVu[W5iYoLvcoNpcWGuIHXwbZRp\WyrYXygZ4VtdHNiYomgWZN{cW6pIHPoZY1j\XK|IILlZ49z\GmwZzD0[YNpdmmzdXWsJGVEPTBiPTCwMlAzOiEQvF2u NIrTNYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS0NVAyOyd-MkW0OFExOTN:L3G+
human CFBE41o cells M2\zO2Z2dmO2aX;uJIF{e2G7 MVmxNEBucW6| M1XRN3BwfGWwdHnheIlwdiCxZjDDSnRTKEZ3MEjk[YwhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKGi3bXHuJGNHSkV2MX:gZ4VtdHNiaX7jeYJifGWmIH\vdkAyOCCvaX7zJIlvKHC{ZYPlcoNmKG:oIH\vdpNsd2yrbjDt[YF{fXKnZDDmc5IhPyC|ZXPzJIJ6KFmIUDDoZYxq\GViYYPzZZktKEWFNUCgQUAxNjF{NjFOwG0v NVrEPIJrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxOFg4PjNpPkK5NVQ5PzZ|PD;hQi=>
human bronchial epithelial cells M{fqcGZ2dmO2aX;uJIF{e2G7 NYn4UZRJWG:2ZX70bYF1cW:wIH;mJIh2dWGwIFPGWHIhTjVyOHTlcEBufXSjboSgbY4hcHWvYX6gZpJwdmOqaXHsJIVxcXSqZXzpZYwh[2WubIOgZpkhXXO|aX7nJINp[W2kZYLzJJJm[2:{ZHnu[{B1\WOqbnnxeYUtKEWFNUCgQUAxNjJ|NjFOwG0v MljjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2NEGwNVMoRjJ3NESxNFE{RC:jPh?=
HEK293 cells NFHheFhHfW6ldHnvckBie3OjeR?= NIezTIUyOCCvaX7z NVizVXg4WG:2ZX70bYF1cW:wIH;mJGNHXFJiR{W1NWQhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDpcoN2[mG2ZXSg[o9zKDFyIH3pcpMhcW5icILld4Vv[2Vib3[g[o9ze2uxbHnuJI1m[XO3cnXkJIZweiB{IH3pcpMh[nliWV\QJIhidGmmZTDhd5NigSxiRVO1NEA:KDFwMzFOwG0v MoHrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzNEi3OlMoRjJ7MUS4O|Y{RC:jPh?=
NRK-49F cells NWHQemlWTnWwY4Tpc44h[XO|YYm= MUTJcohq[mm2aX;uJI9nKFSJRj3i[ZRiOS2rbnT1Z4VlKHSxdHHsJINwdGyjZ3XuJIFk[3WvdXzheIlwdiCrbjDyZZQhVlKNLUS5SkBk\WyuczygTWM2OCB;IESg{txONg>? NFOxclU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS2O|E2Pyd-MkW0OlcyPTd:L3G+
DAOY cells MUDxTHRUKGG|c3H5 MorCdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgSGFQYSClZXzsdy=> NIW3NHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 cells MXfxTHRUKGG|c3H5 MWTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDORk1GSmNzIHPlcIx{ MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) cells NGrPUHFyUFSVIHHzd4F6 NI\CW4dyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBOTyB4MzCoOk1VTyCUKTDj[Yxtew>? Ml7yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
RD cells MYTxTHRUKGG|c3H5 MWHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSSEBk\Wyucx?= NVHIXnFjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC cells M4fTXJFJXFNiYYPzZZk> M1nGVJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN? NYfq[mhxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 cells NILmVHpyUFSVIHHzd4F6 NFnDOZdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBU[W:|LUKgZ4VtdHN? NF7aV4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Assay
Methods Test Index PMID
Western blot PPARγ / pERK NLRP3 Rδf508 30498130 25101887
Immunofluorescence F-actin 30498130
体内研究 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。

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度(25°C)

体外

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 392.49
化学式

C24H28N2O3

CAS号 873054-44-5
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04254705 Unknown status Procedure: Rectal Biopsy Cystic Fibrosis Universitaire Ziekenhuizen Leuven|Vertex Pharmaceuticals Incorporated|KU Leuven|University of Lisbon March 1 2020 Not Applicable
NCT03085485 Recruiting Drug: Ivacaftor 150 MG|Drug: Placebo 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 Drug: Cavosonstat|Drug: Placebo Cystic Fibrosis Nivalis Therapeutics Inc. April 2016 Phase 2
NCT02725567 Active not recruiting Drug: ivacaftor Cystic Fibrosis Vertex Pharmaceuticals Incorporated March 2016 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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