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169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  NYPJemJzTnWwY4Tpc44hSXO|YYm= NVT6bFdyOTBizszN M3voTVExKG2rbh?= MXHheYdu\W62czDDSnRTNWSncHXu[IVvfCCrb36geJJidnOyb4L0xsA> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDFyNkiwNUc,OjRzME[4NFE9N2F-
CFBE41o- MlfUSpVv[3Srb36gRZN{[Xl? MmPvNVAhyrWP Mo\RbY5lfWOnczDyc4J2e3RiaX7jdoVie2W|IHnuJIFvcW:wIITyZY5{eG:{dB?= MnmyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ5NkixN|AoRjJ{N{[4NVMxRC:jPh?=
HBE  MWjGeY5kfGmxbjDBd5NigQ>? MXKxNEDDvU1? NHm3bG5ifWevZX70d{BETlSULXTldIVv\GWwdDDhcolwdiC2cnHud5BwenRiYXP0bZZqfHl? NFXBSYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mke2PFE{OCd-MkK3OlgyOzB:L3G+
HBE  Mn;wSpVv[3Srb36gRZN{[Xl? NWLPVY96OTBiwsXN M3\zWlI1KGh? NWHnUHhOcW6mdXPld{BiKG2xZHXzeEBjfXRic3nncolncWOjboSgbY5kemWjc3WgbY4hSVOOIHTldJRp NIS5NGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mke2PFE{OCd-MkK3OlgyOzB:L3G+
HBE  NGnVXmRHfW6ldHnvckBCe3OjeR?= MV2xNEDDvU1? MYDwc5RmdnSrYYTld{BETlSULXTldIVv\GWwdDDJd4MtKHKnZ3Hy[Ixme3Nib3[gdJJqd3JiYXTtbY5qe3S{YYTpc44hd2ZiQ2PF M2[zfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{N{[4NVMxLz5{Mke2PFE{ODxxYU6=
HBE  MWnGeY5kfGmxbjDBd5NigQ>? MXGxNEDDvU1? NV7IWZVueGG{dHnhcIx6KHKnc4TvdoV{KGSncHzleIlwdiCxZjDBV2wh\GWydHigbY4hS1OHIITy[YF1\WRibX;uc4xigWW{cx?= NU[2UohJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3OlgyOzBpPkKyO|Y5OTNyPD;hQi=>
mouse NIH-3T3 cells MXTGeY5kfGmxbjDhd5NigQ>? MYOzNEBucW6| MV;Qc5RmdnSrYYTpc44hd2ZiaIXtZY4hS0[WUjDGOVA5\GWuIH31eIFvfCCneIDy[ZN{\WRiaX6gcY92e2ViTlnIMVNVOyClZXzsd{Bi\nSncjCzNEBucW6|IHL5JIZtfW:{ZYPj[Y51KH[xbITh[4Uhe2Wwc3nu[{BweHSrY3HsJIF{e2G7LDDFR|UxKD1iMD6wNFMh|ryPLh?= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR2MUCxN{c,OjV2NEGwNVM9N2F-
human bronchial epithelial cells MoPmSpVv[3Srb36gZZN{[Xl? NI\4NItRd3SnboTpZZRqd25ib3[gbJVu[W5iQ1\UVkBHPTB6ZHXsM2c2PTGGIH31eIFvfCCrbjDoeY1idiCkcn;uZ4hq[WxiZYDpeIhmdGmjbDDj[YxteyCkeTDVd5NqdmdiY3jhcYJmenNicnXjc5JlcW6pIITlZ4hvcXG3ZTygSWM2OCB;IECuNFIzKM7:TT6= NGLaS3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS0NVAyOyd-MkW0OFExOTN:L3G+
human CFBE41o cells MkDkSpVv[3Srb36gZZN{[Xl? NFSyUGYyOCCvaX7z NEPT[FdRd3SnboTpZZRqd25ib3[gR2ZVWiCINUC4[IVtKG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCqdX3hckBETkKHNEHvJINmdGy|IHnuZ5Vj[XSnZDDmc5IhOTBibXnud{BqdiCycnXz[Y5k\SCxZjDmc5J{c2:uaX6gcYVie3W{ZXSg[o9zKDdic3Xjd{BjgSC\RmCgbIFtcWSnIHHzd4F6NCCHQ{WwJF0hOC5zMk[g{txONg>? NFzVTYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG0PFc3Oyd-MkmxOFg4PjN:L3G+
human bronchial epithelial cells MUTGeY5kfGmxbjDhd5NigQ>? MnnuVI91\W62aXH0bY9vKG:oIHj1cYFvKEOIVGKgSlUxQGSnbDDteZRidnRiaX6gbJVu[W5iYoLvcoNpcWGuIHXwbZRp\WyrYXygZ4VtdHNiYomgWZN{cW6pIHPoZY1j\XK|IILlZ49z\GmwZzD0[YNpdmmzdXWsJGVEPTBiPTCwMlI{PiEQvF2u MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR2MUCxN{c,OjV2NEGwNVM9N2F-
HEK293 cells NIPJcJZHfW6ldHnvckBie3OjeR?= NIG4[lAyOCCvaX7z MoHzVI91\W62aXH0bY9vKG:oIFPGWHIhTzV3MVSgcZV1[W62IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCrbnP1ZoF1\WRiZn;yJFExKG2rboOgbY4heHKnc3XuZ4Uhd2ZiZn;yd4twdGmwIH3lZZN2emWmIH\vdkAzKG2rboOgZpkhYU[SIHjhcIll\SCjc4PhfUwhTUN3MDC9JFEvOyEQvF2u NXqzSlRXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxOFg4PjNpPkK5NVQ5PzZ|PD;hQi=>
NRK-49F cells NVn1Noc{TnWwY4Tpc44h[XO|YYm= NECzNIpKdmirYnn0bY9vKG:oIGTHSk1j\XSjMT3pcoR2[2WmIITveIFtKGOxbHzh[4VvKGGlY4XteYxifGmxbjDpckBz[XRiTmLLMVQ6TiClZXzsd{whUUN3MDC9JFQh|ryPLh?= Mo[wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2NkexOVcoRjJ3NE[3NVU4RC:jPh?=
DAOY cells NXT4b486eUiWUzDhd5NigQ>? NGjMT5NyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBFSU:\IHPlcIx{ M{PiR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 cells NWXObWRseUiWUzDhd5NigQ>? MVLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDORk1GSmNzIHPlcIx{ M3PHR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) cells MWTxTHRUKGG|c3H5 NHrEe5RyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBOTyB4MzCoOk1VTyCUKTDj[Yxtew>? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD cells MnrGdWhVWyCjc4PhfS=> NWnaXGxweUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhWkRiY3XscJM> M3e1U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC cells NF;HcXdyUFSVIHHzd4F6 NH7iXG9yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUy2QLV3DJINmdGy| NGL1RmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Saos-2 cells MnPXdWhVWyCjc4PhfS=> MUfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTZY9{NTJiY3XscJM> M{X1NVxiKHSjcnfleF0oZ2KuYX7rK{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、SDS / 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、SDS / 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