A5047-5mg | Ivacaftor (VX-770) [873054-44-5] Clinisciences

Background

Ivacaftor (VX-770) is a potent and orally bioavailable small molecule potentiator of cystic fibrosis transmembrane conductance regulator (CFTR). Studies in both G551D- and F508del-CFTR expressing cells have shown VX-700 combined with forskolin, but not VX-700 alone, has significantly increased CFTR-mediated Cl-secretion. The EC50 values of VX-700 in G551D- and F508del-CFTR are 100 nM and 25 nM, respectively ^[1].

VX-770 has been reported to reduce ENaC-mediated Na+ absorption and increase the amount of fluid on the apical surface in human CF bronchial epithelia (HBE) carrying G551D/F508del ^[1]. VX-770 combined with OAG has been shown to increase G551D-CFTR activity and OAG-dependent Ca2+ inﬂux and in Chinese hamster ovary (CHO) cells ^[2].

References:
1. Van Goor F1, Hadida S, Grootenhuis PD, Burton B, Cao D, Neuberger T, Turnbull A, Singh A, Joubran J, Hazlewood A, Zhou J, McCartney J,Arumugam V, Decker C, Yang J, Young C, Olson ER, Wine JJ, Frizzell RA, Ashlock M, Negulescu P. Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770. Proc Natl Acad Sci U S A. 2009 Nov 3;106(44):18825-30.
2. 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

Product Citation

1. Phua YL, Chen KH, et al. "Loss of miR-17~92 results in dysregulation of Cftr in nephron progenitors." Am J Physiol Renal Physiol. 2019 May 1;316(5):F993-F1005. PMID:30838872

Chemical Properties

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.

Protocol

Cell experiment [1]:
Cell lines	CHO-G551D cells
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.
Reaction Conditions	10 μM; 0 ~ 8 mins
Applications	In CHO-G551D cells, VX-770 activated G551D-CFTR channel, and OAG + VX-770 increased G551D-CFTR activity by 58%.
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.

Biological Activity

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

Purity = 98.18%

Related Biological Data

Ivacaftor inhibits mutant CFTR.

Ivacaftor (VX-770) [873054-44-5]

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Background

Product Citation

Chemical Properties

Protocol

Biological Activity

Quality Control

Related Biological Data

Related Biological Data

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