Ambeed 大中华区 CN | ZH

中文 - ZH English - EN

Ambeed.cn

搜索

关键字搜索批量搜索

首页 收藏 购物车0
首页 / 抑制剂/激动剂 / 膜转运蛋白 / CFTR / Ivacaftor/依伐卡托

Ivacaftor/依伐卡托 {[allProObj[0].p_purity_real_show]}

货号：A286566 同义名： 依伐卡托 (VX-770) / VX-770

Ivacaftor 是一种 CFTR 增效剂，对 G551D-CFTR 与 F508del-CFTR 的 EC₅₀ 分别为 100 nM 与 25 nM，广泛用于囊性纤维化的研究。

Ivacaftor/依伐卡托 化学结构 CAS号：873054-44-5
Ivacaftor/依伐卡托 化学结构
CAS号：873054-44-5
Ivacaftor/依伐卡托 3D分子结构
CAS号：873054-44-5
Ivacaftor/依伐卡托 化学结构 CAS号：873054-44-5
Ivacaftor/依伐卡托 3D分子结构 CAS号：873054-44-5
规格 价格 会员价 库存 数量
{[ item.pr_size ]}

{[ getRatePriceInt(item.pr_rmb, 1,1) ]}

{[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}

{[ getRatePriceInt(item.pr_rmb, 1,1) ]}

{[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} 		{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]} 现货 1周 咨询 - +
购物车0 收藏 询单

Ivacaftor/依伐卡托 纯度/质量文件 产品仅供科研

货号：A286566 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025, 188, (21): 5847-5861.e11. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025, 20, 1502-1513. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
产品名称 CFTR ↓ 其他靶点 纯度
Ataluren ✔ 98%
Lumacaftor ++++

F508del-CFTR, EC50: 0.1 μM

 		98%
CFTR(inh)-172 +++

CFTR, Ki: 300 nM

 		99%+
GlyH-101 +

CFTR, Ki: 4.3 μM

 		99%+
IOWH-032 ++

CFTR, IC50: 1.01 μM

 		99%+
Tezacaftor ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Ivacaftor/依伐卡托 生物活性

描述 Cystic fibrosis transmembrane conductance regulator (CFTR) is a protein kinase A-activated epithelial anion channel that is responsible for salt and fluid transport in multiple organs. Ivacaftor is a potent potentiator of CFTR. It increases forskolin-stimulated CFTR-mediated transepithelial current (IT) with an EC50 of 100 ± 47 nM in G551D-FRT cells. Also in F508del-FRT cells, ivacaftor increased forskolin-stimulated IT with an EC50 of 25 ± 5 nM. In recombinant cells expressing G551D-, F508del-, or wild-type (WT)-CFTR, 10 μM ivacaftor increased their CFTR channel open probability by ~6-fold, ~5-fold and ~2-fold, respectively. Treatment of ivacaftor significantly increased the forskolin-stimulated IT in F508del human bronchial epithelia (HBE) cells with an EC50 of 22 ± 10 nM. G551D/F508del HBE cells treated with 10μM ivacaftor for 5 days showed significant increased cilia beat frequency compared with vehicle-treated controls[1]. In the analysis of ATP-independent activity for WT-CFTR, 200 nM ivacaftor increased the activity by 2-fold, as determined by the ratio of post washout ATP-independent current to the robust ATP-induced current[2]. The bilayer studies of WT-CFTR showed that the open probability of CFTR channel treated with both 1 mM Mg-ATP and 2 μM ivacaftor was approximately twice that measured in the presence of Mg-ATP alone. The treatment of 10 μM ivacaftor on liposomes containing phosphorylated F508del-CFTR or phosphorylated G551D-CFTR increased iodide-mediated flux in the presence of 1 mM Mg-ATP[3].
作用机制 Ivacaftor potentiates CFTR function by increasing the open time of WT-CFTR, stabilizing a post-hydrolytic open state, thereby promoting decoupling between the gating cycle and ATP hydrolysis cycle[2].

Ivacaftor/依伐卡托 细胞实验

Cell Line
Concentration Treated Time Description References
human corneal epithelial cells (pHCECs) 10 µM 72 h To evaluate the effect of Ivacaftor on EXOA-induced P38 phosphorylation and cell death in CF cells, results showed that Ivacaftor significantly reduced P38 phosphorylation and decreased EXOA-induced cell death in CF cells. J Exp Med. 2023 Oct 2;220(10):e20230104.
human nasal epithelial cells (pHNECs) 10 µM 72 h To evaluate the effect of Ivacaftor on EXOA-induced P38 phosphorylation and cell death in CF cells, results showed that Ivacaftor significantly reduced P38 phosphorylation and decreased EXOA-induced cell death in CF cells. J Exp Med. 2023 Oct 2;220(10):e20230104.
16HBEge cells 1 µM 72 h Used to activate CFTR channels and measure CFTR-mediated chloride current changes. Nat Commun. 2021 Jul 16;12(1):4358.
Calu-3 2B4 cells 5 µM 48 h To evaluate the effect of Ivacaftor on SARS-CoV-2 replication, results showed that Ivacaftor treatment significantly reduced virus titers. mBio. 2023 Feb 28;14(1):e0313622.

Ivacaftor/依伐卡托 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice K18-hACE2 mice Intraperitoneal injection 6 mg/kg Once daily for 8 days To evaluate the protective effect of Ivacaftor in SARS-CoV-2 infected mice, results showed that Ivacaftor treatment significantly improved survival and reduced lung edema. mBio. 2023 Feb 28;14(1):e0313622.
Mice BALB/CJ mice Subcutaneous injection 50 mg/kg Single injection, lasting 28 days To study the pharmacokinetics of Ivacaftor-loaded PLGA microparticles in mice, the results showed that the microparticle formulation maintained stable plasma drug concentrations for 28 days, with a 6-fold increase in AUC compared to intravenous administration of solubilized Ivacaftor. Int J Pharm. 2024 Jan 25;650:123693

Ivacaftor/依伐卡托 动物研究

Dose Rat: 10 mg/kg - 50 mg/kg[4] (p.o.) Dog: 60 mg/kg[4] (p.o.)
Administration p.o.

Ivacaftor/依伐卡托 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03525548 Cystic Fibrosis Phase 3 Active, not recruiting March 2019 -
NCT03447249 Cystic Fibrosis Phase 3 Active, not recruiting April 16, 2019 -
NCT03525574 Cystic Fibrosis Phase 3 Enrolling by invitation June 2021 -

Ivacaftor/依伐卡托 参考文献

[1]Van Goor F, Hadida S, et al. Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770. Proc Natl Acad Sci U S A. 2009;106(44):18825-30.

[2]Jih KY, Hwang TC. Vx-770 potentiates CFTR function by promoting decoupling between the gating cycle and ATP hydrolysis cycle. Proc Natl Acad Sci U S A. 2013;110(11):4404-9.

[3]Eckford PD, Li C, et al. Cystic fibrosis transmembrane conductance regulator (CFTR) potentiator VX-770 (ivacaftor) opens the defective channel gate of mutant CFTR in a phosphorylation-dependent but ATP-independent manner. J Biol Chem. 2012;287(44):36639-49.

Ivacaftor/依伐卡托 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.25mL

12.74mL

2.55mL

1.27mL

25.48mL

5.10mL

2.55mL

Ivacaftor/依伐卡托 技术信息

CAS号873054-44-5
分子式C24H28N2O3
分子量 392.49
SMILES Code O=C(C1=CNC2=C(C=CC=C2)C1=O)NC3=CC(O)=C(C(C)(C)C)C=C3C(C)(C)C
MDL No. MFCD17171361
别名 依伐卡托 (VX-770) ;VX-770
运输蓝冰
InChI Key PURKAOJPTOLRMP-UHFFFAOYSA-N
Pubchem ID 16220172
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C
溶解方案

DMSO: 50 mg/mL(127.39 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Ivacaftor | 873054-44-5 | VX-770 | VX770 | VX 770 | Membrane Transporter/Ion Channel | Autophagy | CFTR | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Ivacaftor/依伐卡托 纯度/质量文件 | Ivacaftor/依伐卡托 亚型比较 | Ivacaftor/依伐卡托 生物活性 | Ivacaftor/依伐卡托 动物研究 | Ivacaftor/依伐卡托 临床数据 | Ivacaftor/依伐卡托 参考文献 | Ivacaftor/依伐卡托 实验方案 | Ivacaftor/依伐卡托 技术信息

AmBeed 相关网站 AmBeed.cn AmBeed.com
AmBeed
关于我们
联系我们
资讯中心
网站地图
产品手册
  • 批次文件查询
    • 客户支持
    技术支持
    专业术语
    缩略词释义
    质量手册
    产品咨询
    计算器
    活动政策
    订购方法
    积分商城
    活动声明
    联系我们
    400-920-2911 sales@ambeed.cn tech@ambeed.cn
    AmBeed 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质用途提供服务。

    尊敬的 AmBeed 客户您好，
    请您选择所在区域，我们将转接对应客服为您服务！

    热门区域

    A

    B

    C

    F

    G

    H

    J

    L

    N

    Q

    S

    T

    X

    Y

    Z

    热 A B C F G H J L N Q S T X Y Z