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149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  M4HKeWZ2dmO2aX;uJGF{e2G7 MofXNVAh|ryP NX;Jc2dvOTBibXnu MmL2ZZVodWWwdIOgR2ZVWi2mZYDlcoRmdnRiaX;uJJRz[W6|cH;yeOKh NIi5WlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGwOlgxOSd-MkSxNFY5ODF:L3G+
CFBE41o- M3yzO2Z2dmO2aX;uJGF{e2G7 NXW3THpGOTBiwsXN MYnpcoR2[2W|IILvZpV{fCCrbnPy[YF{\XNiaX6gZY5qd25idILhcpNxd3K2 MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjd4OEGzNEc,OjJ5NkixN|A9N2F-
HBE  NHzxZmVHfW6ldHnvckBCe3OjeR?= NXv3V3o3OTBiwsXN M4jZWIF2\22nboTzJGNHXFJvZHXw[Y5l\W62IHHubY9vKHS{YX7zdI9zfCCjY4Tpeol1gQ>? NX\3dXFQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3OlgyOzBpPkKyO|Y5OTNyPD;hQi=>
HBE  MUDGeY5kfGmxbjDBd5NigQ>? Mlq2NVAhyrWP NET1V2QzPCCq NGXUXGZqdmS3Y3XzJIEhdW:mZYP0JIJ2fCC|aXfubYZq[2GwdDDpcoNz\WG|ZTDpckBCW0xiZHXweIg> NYK3cHhnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3OlgyOzBpPkKyO|Y5OTNyPD;hQi=>
HBE  NGHZTVBHfW6ldHnvckBCe3OjeR?= NX;CT5BrOTBiwsXN MnHvdI91\W62aXH0[ZMhS0[WUj3k[ZBmdmSnboSgTZNkNCC{ZXfhdoRt\XO|IH;mJJBzcW:{IHHkcYlvcXO2cnH0bY9vKG:oIFPTSS=> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjd4OEGzNEc,OjJ5NkixN|A9N2F-
HBE  M4e5[WZ2dmO2aX;uJGF{e2G7 M2X3ZlExKML3TR?= Mm\PdIFzfGmjbHz5JJJme3SxcnXzJIRmeGyndHnvckBw\iCDU1yg[IVxfGhiaX6gR3NGKHS{ZXH0[YQhdW:wb3zhfYVzew>? MoS3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ5NkixN|AoRjJ{N{[4NVMxRC:jPh?=
mouse NIH-3T3 cells MWrGeY5kfGmxbjDhd5NigQ>? MUezNEBucW6| Mn\lVI91\W62aXH0bY9vKG:oIHj1cYFvKEOIVGKgSlUxQGSnbDDteZRidnRiZYjwdoV{e2WmIHnuJI1wfXOnIF7JTE0{XDNiY3XscJMh[W[2ZYKgN|AhdWmwczDifUBndHWxcnXzZ4VvfCC4b3z0ZYdmKHOnboPpcochd3C2aXPhcEBie3OjeTygSWM2OCB;IECuNFA{KM7:TT6= NU\ueWdVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0OFExOTNpPkK1OFQyODF|PD;hQi=>
human bronchial epithelial cells NHXFZ41HfW6ldHnvckBie3OjeR?= MXvQc5RmdnSrYYTpc44hd2ZiaIXtZY4hS0[WUjDGOVA5\GWuL1e1OVFFKG23dHHueEBqdiCqdX3hckBjem:wY3jpZYwh\XCrdHjlcIlidCClZXzsd{BjgSCXc4Ppcoch[2ijbXLldpMhemWlb4LkbY5oKHSnY3jubZF2\SxiRVO1NEA:KDBwMEKyJO69VS5? M2jEPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NESxNFE{Lz5{NUS0NVAyOzxxYU6=
human CFBE41o cells MnvoSpVv[3Srb36gZZN{[Xl? MnHHNVAhdWmwcx?= MXzQc5RmdnSrYYTpc44hd2ZiQ1\UVkBHPTB6ZHXsJI12fGGwdDCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBpfW2jbjDDSmJGPDGxIHPlcIx{KGmwY4XiZZRm\CCob4KgNVAhdWmwczDpckBxemW|ZX7j[UBw\iCob4Lzb49tcW5ibXXhd5Vz\WRiZn;yJFche2WlczDifUB[TlBiaHHsbYRmKGG|c3H5MEBGSzVyIE2gNE4yOjZizszNMi=> MnLQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzNEi3OlMoRjJ7MUS4O|Y{RC:jPh?=
human bronchial epithelial cells MkTvSpVv[3Srb36gZZN{[Xl? NYT6W|lDWG:2ZX70bYF1cW:wIH;mJIh2dWGwIFPGWHIhTjVyOHTlcEBufXSjboSgbY4hcHWvYX6gZpJwdmOqaXHsJIVxcXSqZXzpZYwh[2WubIOgZpkhXXO|aX7nJINp[W2kZYLzJJJm[2:{ZHnu[{B1\WOqbnnxeYUtKEWFNUCgQUAxNjJ|NjFOwG0v M37W[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NESxNFE{Lz5{NUS0NVAyOzxxYU6=
HEK293 cells MnX6SpVv[3Srb36gZZN{[Xl? M3rvTlExKG2rboO= MULQc5RmdnSrYYTpc44hd2ZiQ1\UVkBIPTVzRDDteZRidnRiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGmwY4XiZZRm\CCob4KgNVAhdWmwczDpckBxemW|ZX7j[UBw\iCob4Lzb49tcW5ibXXhd5Vz\WRiZn;yJFIhdWmwczDifUB[TlBiaHHsbYRmKGG|c3H5MEBGSzVyIE2gNU4{KM7:TT6= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2OEe2N{c,OjlzNEi3OlM9N2F-
NRK-49F cells NGjwS4tHfW6ldHnvckBie3OjeR?= M17rcmlvcGmkaYTpc44hd2ZiVFfGMYJmfGFzLXnu[JVk\WRidH;0ZYwh[2:ubHHn[Y4h[WOldX31cIF1cW:wIHnuJJJifCCQUlutOFlHKGOnbHzzMEBKSzVyIE2gOEDPxE1w MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR4N{G1O{c,OjV2NkexOVc9N2F-
DAOY cells M4HmWpFJXFNiYYPzZZk> NHzTeYdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBFSU:\IHPlcIx{ MkDkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1 cells MnLodWhVWyCjc4PhfS=> MXXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDORk1GSmNzIHPlcIx{ Mnf3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) cells MYLxTHRUKGG|c3H5 M3zQ[pFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJG1IKDZ|IDi2MXRIKFJrIHPlcIx{ MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD cells NGT6eolyUFSVIHHzd4F6 M3uyW5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJFKGOnbHzz Ml;jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC cells NHT2OZFyUFSVIHHzd4F6 MWHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTT{1PNU2FIHPlcIx{ MkfrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 cells NEjjO4FyUFSVIHHzd4F6 MlPTdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV4Fwey1{IHPlcIx{ M2XaSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... 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