Ivacaftor

Name: Ivacaftor
Brand: Tocris Bioscience
SKU: 7887

Tocris Bioscience, part of Bio-Techne | Catalog # 7887

COA / SDS

Potent and selective CFTR potentiator

Key Product Details

Description:	Potent and selective CFTR potentiator
Chemical Name:	N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-3-quinolinecarboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	392.5

View Full Technical Details for Ivacaftor

Technical Data
Citations

Biological Activity for Ivacaftor

Ivacaftor is a potent and selective potentiator of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) that targets F508del-CFTR and G551D-CFTR (EC₅₀ values are 25 nM and 100 nM, respectively); its potentiation activity depends on the level of CFTR phosphorylation. Ivacaftor reversibly binds to wild type (WT-CFTR) and G551D-CFTR mutants, increasing the open probability via an ATP-independent mechanism, and enhances cAMP/PKA-signaling mediated gating activity for both WT-CFTR and G551D-CFTR mutants. In cultured human CF bronchial epithelia with G551D/F508del mutations, Ivacaftor increases Forskolin (Cat. No. 1099)-induced transepithelial current (EC₅₀ = 236 nM) and increases chloride secretion by 10-fold. Also rescues endothelial CFTR expression and function and prevents endothelial barrier failure and protein leak in human pulmonary microvascular endothelial cells. Ivacaftor is orally bioavailable.

Technical Data for Ivacaftor

M. Wt	392.5
Formula	C₂₄H₂₈N₂O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	873054-44-5
PubChem ID	16220172
InChi Key	PURKAOJPTOLRMP-UHFFFAOYSA-N
Smiles	O=C(C1=CNC2=C(C1=O)C=CC=C2)NC3=CC(O)=C(C(C)(C)C)C=C3C(C)(C)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Ivacaftor

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	ethanol	1.96	5
	DMSO	39.25	100

Preparing Stock Solutions for Ivacaftor

The following data is based on the product molecular weight 392.5.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.55 mL	12.74 mL	25.48 mL
5 mM	0.51 mL	2.55 mL	5.10 mL
10 mM	0.25 mL	1.27 mL	2.55 mL
50 mM	0.05 mL	0.25 mL	0.51 mL

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References for Ivacaftor

References are publications that support the biological activity of the product.

Nguyen Modulation of cAMP metabolism for CFTR potentiation in human airway epithelial cells. Sci.Rep. 2021 PMID: 33441643
Eckford 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. J.Biol.Chem. 2012 PMID: 22942289
Levring CFTR function, pathology and pharmacology at single-molecule resolution. Nature 2023 PMID: 36949202
Erfinanda Loss of endothelial CFTR drives barrier failure and edema formation in lung infection and can be targeted by CFTR potentiation. Sci.Transl.Med. 2022 PMID: 36475904
Cui VX-770-mediated potentiation of numerous human CFTR disease mutants is influenced by phosphorylation level. Sci.Rep. 2019 PMID: 31530897
Jih Vx-770 potentiates CFTR function by promoting decoupling between the gating cycle and ATP hydrolysis cycle. Proc.Natl.Acad.Sci.U.S.A. 2013 PMID: 23440202