Ivacaftor (VX-770)

For research use only. Not for use in humans.

目录号:S1144 中文名称:依伐卡托

Ivacaftor (VX-770) Chemical Structure

CAS No. 873054-44-5

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。

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 2608.67 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153篇:

产品安全说明书

CFTR抑制剂选择性比较

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  MonDSpVv[3Srb36gRZN{[Xl? NFrlc4YyOCEQvF2= MnTPNVAhdWmw NWO3b4VI[XWpbXXueJMhS0[WUj3k[ZBmdmSnboSgbY9vKHS{YX7zdI9zfMLi M1\GblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUC2PFAyLz5{NEGwOlgxOTxxYU6=
CFBE41o- NUHZZ5JqTnWwY4Tpc44hSXO|YYm= MXSxNEDDvU1? NF\ONVNqdmS3Y3XzJJJw[nW|dDDpcoNz\WG|ZYOgbY4h[W6rb36geJJidnOyb4L0 MoLvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ5NkixN|AoRjJ{N{[4NVMxRC:jPh?=
HBE  M{njd2Z2dmO2aX;uJGF{e2G7 NF3GUZoyOCEEtV2= NYXx[GVs[XWpbXXueJMhS0[WUj3k[ZBmdmSnboSgZY5qd25idILhcpNxd3K2IHHjeIl3cXS7 MoTzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ5NkixN|AoRjJ{N{[4NVMxRC:jPh?=
HBE  NEDMOFhHfW6ldHnvckBCe3OjeR?= NFL4U|IyOCEEtV2= MV6yOEBp M{jPWIlv\HWlZYOgZUBud2Snc4SgZpV1KHOrZ37p[olk[W62IHnuZ5Jm[XOnIHnuJGFUVCCmZYD0bC=> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjd4OEGzNEc,OjJ5NkixN|A9N2F-
HBE  Mnq3SpVv[3Srb36gRZN{[Xl? MnrZNVAhyrWP MVLwc5RmdnSrYYTld{BETlSULXTldIVv\GWwdDDJd4MtKHKnZ3Hy[Ixme3Nib3[gdJJqd3JiYXTtbY5qe3S{YYTpc44hd2ZiQ2PF NEm0WlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mke2PFE{OCd-MkK3OlgyOzB:L3G+
HBE  NUTUbHkzTnWwY4Tpc44hSXO|YYm= NXOwRXdWOTBiwsXN NGHadXdx[XK2aXHscJkhemW|dH;y[ZMh\GWybHX0bY9vKG:oIFHTUEBl\XC2aDDpckBEW0VidILlZZRm\CCvb37vcIF6\XK| MnfPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ5NkixN|AoRjJ{N{[4NVMxRC:jPh?=
mouse NIH-3T3 cells M2PaNWZ2dmO2aX;uJIF{e2G7 MYGzNEBucW6| NEDCW4dRd3SnboTpZZRqd25ib3[gbJVu[W5iQ1\UVkBHPTB6ZHXsJI12fGGwdDDlfJBz\XO|ZXSgbY4hdW:3c3WgUmlJNTOWMzDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KG[udX;y[ZNk\W62II\vcJRi\2Vic3Xud4lv\yCxcITpZ4FtKGG|c3H5MEBGSzVyIE2gNE4xODNizszNMi=> NILMXmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS0NVAyOyd-MkW0OFExOTN:L3G+
human bronchial epithelial cells MYnGeY5kfGmxbjDhd5NigQ>? NVnINHVnWG:2ZX70bYF1cW:wIH;mJIh2dWGwIFPGWHIhTjVyOHTlcE9IPTVzRDDteZRidnRiaX6gbJVu[W5iYoLvcoNpcWGuIHXwbZRp\WyrYXygZ4VtdHNiYomgWZN{cW6pIHPoZY1j\XK|IILlZ49z\GmwZzD0[YNpdmmzdXWsJGVEPTBiPTCwMlAzOiEQvF2u NIjMTpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS0NVAyOyd-MkW0OFExOTN:L3G+
human CFBE41o cells MknKSpVv[3Srb36gZZN{[Xl? MVyxNEBucW6| NYXvdVFZWG:2ZX70bYF1cW:wIH;mJGNHXFJiRkWwPIRmdCCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iaIXtZY4hS0[ERUSxc{Bk\WyuczDpcoN2[mG2ZXSg[o9zKDFyIH3pcpMhcW5icILld4Vv[2Vib3[g[o9ze2uxbHnuJI1m[XO3cnXkJIZweiB5IIPlZ5Mh[nliWV\QJIhidGmmZTDhd5NigSxiRVO1NEA:KDBwMUK2JO69VS5? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2OEe2N{c,OjlzNEi3OlM9N2F-
human bronchial epithelial cells M33RNmZ2dmO2aX;uJIF{e2G7 M17JWnBwfGWwdHnheIlwdiCxZjDoeY1idiCFRmTSJGY2ODimZXygcZV1[W62IHnuJIh2dWGwIHLyc45kcGmjbDDldIl1cGWuaXHsJINmdGy|IHL5JHV{e2mwZzDjbIFu[mW{czDy[YNwemSrbnegeIVkcG6rcYXlMEBGSzVyIE2gNE4zOzZizszNMi=> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR2MUCxN{c,OjV2NEGwNVM9N2F-
HEK293 cells M{TRRWZ2dmO2aX;uJIF{e2G7 MmrGNVAhdWmwcx?= NFLMNWRRd3SnboTpZZRqd25ib3[gR2ZVWiCJNUWxSEBufXSjboSgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHnuZ5Vj[XSnZDDmc5IhOTBibXnud{BqdiCycnXz[Y5k\SCxZjDmc5J{c2:uaX6gcYVie3W{ZXSg[o9zKDJibXnud{BjgSC\RmCgbIFtcWSnIHHzd4F6NCCHQ{WwJF0hOS5|IN88UU4> NVLpdZNNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxOFg4PjNpPkK5NVQ5PzZ|PD;hQi=>
NRK-49F cells MnzpSpVv[3Srb36gZZN{[Xl? MmrZTY5pcWKrdHnvckBw\iCWR1[tZoV1[TFvaX7keYNm\CC2b4ThcEBkd2yuYXflckBi[2O3bYXsZZRqd25iaX6gdoF1KE6USz20PWYh[2WubIOsJGlEPTBiPTC0JO69VS5? NH:ydFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS2O|E2Pyd-MkW0OlcyPTd:L3G+
DAOY cells M{S2UpFJXFNiYYPzZZk> Ml\SdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgSGFQYSClZXzsdy=> MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB-EBc1 cells MUHxTHRUKGG|c3H5 MYTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDORk1GSmNzIHPlcIx{ NGHIbWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
MG 63 (6-TG R) cells Mnf4dWhVWyCjc4PhfS=> NY\OWpBPeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? MkK0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
RD cells NFj5XoFyUFSVIHHzd4F6 M1SyV5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJFKGOnbHzz M4jGRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC cells M4WwN5FJXFNiYYPzZZk> M3nVTJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN? MoG0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 cells M{naSZFJXFNiYYPzZZk> Mn6zdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV4Fwey1{IHPlcIx{ MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
PPARγ / pERK; 

PubMed: 30498130     


Caco-2 cells incubated with P31–43 in the presence or absence of VX-770. Immunoblot of PPARc or phospho-ERK1/2 (phERK1/2) and densitometric analysis of protein levels relative to b-actin.

NLRP3; 

PubMed: 30498130     


Immunoblotting with specific antibodies (NLRP3) in Caco-2 cells challenged for 2 or 4 h in the presence or absence of VX-770. NLRP3 expression.

Rδf508; 

PubMed: 25101887     


Effect of VX-770 on the expression pattern of low temperature-rescued ΔF508-CFTR-3HA determined by immunoblot. Cells were treated with VX-770 alone for 24 hours at 26°C. CFTR was visualized with anti-HA antibody, and anti–Na+/K+-ATPase antibody served as loading control. 

30498130 25101887
Immunofluorescence
F-actin; 

PubMed: 30498130     


Confocal image staining with anti-F-actin. DAPI (blue), nuclear counterstaining. Scale bar, 50 μm.

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 DMSO 78 mg/mL (198.73 mM)
Water Insoluble
Ethanol Insoluble

* 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 粉状
溶于溶剂
别名 N/A

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04254705 Not yet recruiting 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 Recruiting Drug: ivacaftor Cystic Fibrosis Vertex Pharmaceuticals Incorporated March 2016 Phase 3

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CFTR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID