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VX-770 (Ivacaftor)

Cat. No. M1854
VX-770 (Ivacaftor) Structure
Synonym:

Ivacaftor

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 55  USD55 In stock
5mg USD 55  USD55 In stock
10mg USD 90  USD90 In stock
50mg USD 180  USD180 In stock
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Quality Control & Documentation
Biological Activity

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.

Customer Product Validations & Biological Datas
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.
Protocol (for reference only)
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Eckford PD, et al. J Biol Chem. 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.

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  Catalog
Abmole Inhibitor Catalog




Keywords: VX-770 (Ivacaftor), Ivacaftor supplier, CFTR, inhibitors, activators


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