Ivacaftor (VX-770) is a selective enhancer of CFTR that targets G551D-CFTR and F508del-CFTR, with EC50 of 100 nM and 25 nM, respectively, in fisher rat thyrocytes.

 

Brand: BCM

 

Target: CFTR; Autophagy

 

Signaling Pathways: Autophagy; Membrane transporter/Ion channel

 

In Vitro: VX-770 increased the forskolin-stimulated IT in temperature-corrected F508del-FRT cells by ~6-fold with an EC50 of 25 ± 5 nM. Before the addition of VX-770, the CFTR channel was exposed to maximally effective concentrations of PKA (75 nM) and ATP (1 mM). Under these conditions, 10 μM VX-770 increased the Po of G551D CFTR by ~6-fold. HEK293 cells transiently expressing ABCB4-wt or the mutants were treated with 10 μmol/L of ivacaftor (VX-770), for 24 hours. Treatment with ivacaftor increased the PC secretion activity by 3-fold for ABCB4-G535D, 13.7-fold for ABCB4-G536R, 6.7-fold for ABCB4-S1076C, 9.4-fold for ABCB4-S1176L and 5.7-fold for ABCB4-G1178S.

 

Melting Point: 212-215°C

 

Boiling Point: 550.4±50.0 °C(Predicted)

 

pKa: 11.08±0.23(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethanol.

 

GHS: GHS07, GHS08

 

Isomeric SMILES: CC(C)(C)C1=CC(=C(C=C1NC(=O)C2=CNC3=CC=CC=C3C2=O)O)C(C)(C)C  

 

InChIKey: PURKAOJPTOLRMP-UHFFFAOYSA-N  

 

InChI: InChI=1S/C24H28N2O3/c1-23(2,3)16-11-17(24(4,5)6)20(27)12-19(16)26-22(29)15-13-25-18-10-8-7-9-14(18)21(15)28/h7-13,27H,1-6H3,(H,25,28)(H,26,29)

 

Attribute
[Chem Name]	N-(2,4-ditert-butyl-5-hydroxyphenyl)-4-oxo-1H-quinoline-3-carboxamide
[Synonym]	Ivacaftor; VX-770
[CAS No.]	873054-44-5
[MDL No.]	MFCD17171361
[Formula]	C24H28N2O3
[Molecular]	392.49
[Form]	White to Light Brown Solid
[Storage]	Sealed in dry, 2-8°C

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