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VX-770 (Ivacaftor) is a first-in-class potentiator of CFTR, which targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM, respectively. VX-770 (Ivacaftor) inhibits excessive ENaC-mediated Na+ and fluid absorption with an IC50 of 43 nM, and decreases the amiloride response, resulting in an increase in the surface fluid and cilia beat frequency (CBF) in G551D/F508del HBE. VX-770 (Ivacaftor) is the first potent and orally available CFTR potentiator to enter human clinical trials. It showed that VX-770 (Ivacaftor) was associated with within-subject improvements in CFTR and lung function. These findings provide support for further studies of pharmacologic potentiation of CFTR as a means to treat cystic fibrosis.
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Source | Physiology University of Toronto (2015). Figure 21. VX-770 (AbMole BioScience, Cedarlane, Burlington, Canada) |
| Method | CFTR potentiation | |
| Cell Lines | C57BL/6 WT mice | |
| Concentrations | 100nM | |
| Incubation Time | 30 min | |
| Results | Since CFTR(inh)-172 results in the inhibition of proper CFTR gating leading to an elevated myogenic vasoconstriction, treatment with potentiator VX-770 might also potentiate CFTR’s capacity to transport S1P and, therefore, compensate for part of the lost CFTR. |
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | Iodide Flux Assay—Proteoliposomes were reconstituted in the presence of 75 mM KI. The external iodide was exchanged for 75 mM potassium glutamate by gel filtration chromatography. External iodide concentrations were monitored continuously using an iodide-selective electrode (Lazar Research Laboratories, Los Angeles, CA) interfaced to the Digidata 1320A data acquisi ion system and controlled by Clampex 8 software (Axon Instruments, Sunnyvale, CA), as described previously (17, 18). |
| Concentrations | 10 μM |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 392.49 |
| Formula | C24H28N2O3 |
| CAS Number | 873054-44-5 |
| Solubility (25°C) | DMSO 65 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CFTR Products |
|---|
| Ataluren
Ataluren (PTC124) is a novel, orally available small molecular CFTR-G542X nonsense allele inhibitor. |
| Lonidamine
Lonidamine (AF-1890) is a novel CFTR open channel blocker with an IC50 of 0.85 mM, which inhibits aerobic glycolysis in cancer cells. Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor (Ki=2.5 μM). |
| VX-809
VX-809 is a CFTR corrector that improves CFTR processing and maturation in the cell. |
| CFTR(inh)-172
CFTR(inh)-172 is a voltage-independent, selective CFTR inhibitor with Ki of 300 nM, showing no effects on MDR1, ATP-sensitive K+ channels, or a series of other transporters. |
| IOWH032
IOWH032 is a synthetic CFTR inhibitor with IC50 of 1.01 μM in CHO-CFTR cell based assays. |
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