Ivacaftor (VX-770)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ivacaftor（VX-770）是一种有效的和可口服的囊性纤维化跨膜传导调节器（CFTR）小分子增强剂。在表达G551D-和F508del-CFTR的细胞中，VX-770与forskolin联合使用，而非VX-770单独给药显著增加CFTR介导的Cl-分泌，EC50值分别为100 nM和25 nM[1]。
据报道，在表达G551D/F508del-CFTR的人CF支气管上皮细胞（HBE）中，VX-770减少ENaC介导的Na+吸收，增加表面液体的量[1]。在中国仓鼠卵巢（CHO）细胞中，VX-770与OAG联合使用可以增加G551D-CFTR的活性以及OAG依赖性的Ca2+流入[2]。
参考文献：
1. Van Goor F1, Hadida S, Grootenhuis PD, Burton B, Cao D, Neuberger T, Turnbull A, Singh A, Joubran J, Hazlewood A, Zhou J, McCartney J,Arumugam V, Decker C, Yang J, Young C, Olson ER, Wine JJ, Frizzell RA, Ashlock M, Negulescu P. Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770. Proc Natl Acad Sci U S A. 2009 Nov 3;106(44):18825-30.
2. Vachel L1, Norez C, Becq F, Vandebrouck C. Effect of VX-770 (ivacaftor) and OAG on Ca2+ influx and CFTR activity in G551D and F508del-CFTR expressing cells. J Cyst Fibros. 2013 Dec;12(6):584-91
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 392.49 |
| Cas No. | 873054-44-5 |
| Formula | C24H28N2O3 |
| Solubility | insoluble in H2O; ≥19.6 mg/mL in DMSO; ≥2.95 mg/mL in EtOH with ultrasonic |
| Chemical Name | N-(2,4-ditert-butyl-5-hydroxyphenyl)-4-oxo-1H-quinoline-3-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CC(C)(C)C1=CC(=C(C=C1NC(=O)C2=CNC3=CC=CC=C3C2=O)O)C(C)(C)C |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
CHO-G551D细胞 |
|
制备方法 |
在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液，一般步骤如下：请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
|
反应条件 |
10 μM；0 ~ 8分钟 |
|
实验结果 |
在CHO-G551D细胞中，VX-770活化G551D-CFTR通道。此外，OAG + VX-770增加G551D-CFTR活性（58%）。 |
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References: [1]. Vachel L1, Norez C, Becq F, Vandebrouck C. Effect of VX-770 (ivacaftor) and OAG on Ca2+ influx and CFTR activity in G551D and F508del-CFTR expressing cells. J Cyst Fibros. 2013 Dec;12(6):584-91. | |
| 描述 | Ivacaftor (VX-770)是一种CFTR增强剂，靶向作用于G551D-CFTR和F508del-CFTR，EC50值分别为100 nM和25 nM。 | |||||
| 靶点 | G551D-CFTR | F508del-CFTR | ||||
| IC50 | 100 nM | 25 nM | ||||
质量控制和MSDS
- 批次:
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