Ivacaftor (VX-770)
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.
| 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 |
| Shipping Condition | Small 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. |
| Cell experiment [1]: | |
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Cell lines |
CHO-G551D cells |
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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. |
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Reaction Conditions |
10 μM; 0 ~ 8 mins |
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Applications |
In CHO-G551D cells, VX-770 activated G551D-CFTR channel, and OAG + VX-770 increased G551D-CFTR activity by 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. | |
| 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 & MSDS
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