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Ivacaftor (VX-770)

Catalog No.
A5047
Potent CFTR potentiator
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$61.00
In stock
Evaluation Sample
$30.00
In stock
5mg
$55.00
In stock
25mg
$88.00
In stock
100mg
$149.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Ivacaftor (VX-770; CAS 873054-44-5) is an orally bioavailable small molecule potentiator targeting the cystic fibrosis transmembrane conductance regulator (CFTR). Ivacaftor enhances CFTR-mediated chloride ion transport, especially in cells expressing G551D- or F508del-CFTR mutations. In vitro studies demonstrated that Ivacaftor, in combination with forskolin, significantly increased CFTR-dependent chloride secretion (EC50: 100 nM in G551D-, 25 nM in F508del-expressing cells). Similarly, Ivacaftor reduced ENaC-mediated sodium reabsorption and increased airway surface liquid volume in human cystic fibrosis bronchial epithelial cells. Ivacaftor is utilized in research to investigate CFTR function restoration and associated ion transport processes.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt392.49
Cas No.873054-44-5
FormulaC24H28N2O3
Solubilityinsoluble in H2O; ≥19.6 mg/mL in DMSO; ≥2.95 mg/mL in EtOH with ultrasonic
Chemical NameN-(2,4-ditert-butyl-5-hydroxyphenyl)-4-oxo-1H-quinoline-3-carboxamide
SDFDownload SDF
Canonical SMILESCC(C)(C)C1=CC(=C(C=C1NC(=O)C2=CNC3=CC=CC=C3C2=O)O)C(C)(C)C
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

CHO-G551D cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months.

Reaction Conditions

10 μM; 0 ~ 8 mins

Applications

In CHO-G551D cells, VX-770 activated G551D-CFTR channel, and OAG + VX-770 increased G551D-CFTR activity by 58%.

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.

Biological Activity

Description Ivacaftor (VX-770) is a potentiator of CFTR for G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM, respectively.
Targets G551D-CFTR F508del-CFTR        
IC50 100 nM 25 nM        

Quality Control

Related Biological Data

Ivacaftor
Ivacaftor inhibits mutant CFTR.

Related Biological Data

Ivacaftor