Ivacaftor-d19

Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research[1].

Product Specifications

CAS Number

[1413431-22-7]

Product Name Alternative

VX-770-d19

UNSPSC

12352005

Hazard Statement

H302+H312+H332, H315, H319

Target

Autophagy; CFTR

Type

Isotope-Labeled Compounds

Related Pathways

Autophagy; Membrane Transporter/Ion Channel

Field of Research

Endocrinology

Purity

98.10

Solubility

10 mM in DMSO

Smiles

O=C(C1=CNC2=C(C=CC=C2)C1=O)NC3=CC(O)=C(C(C([2H])([2H])[2H])(C([2H])([2H])[2H])C([2H])([2H])[2H])C([2H])=C3C(C([2H])([2H])[2H])(C([2H])([2H])[2H])C([2H])([2H])[2H]

Molecular Formula

C24H9D19N2O3

Molecular Weight

411.61

Precautions

H302+H312+H332, H315, H319

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]Delaunay JL, et al. Functional defect of variants in the adenosine triphosphate-binding sites of ABCB4 and their rescue by the cystic fibrosis transmembrane conductance regulator potentiator, ivacaftor (VX-770) . Hepatology. 2017 Feb;65 (2) :560-570|[3]Hadida S, et al. Discovery of N- (2,4-di-tert-butyl-5-hydroxyphenyl) -4-oxo-1,4-dihydroquinoline-3-carboxamide (VX-770, ivacaftor), a potent and orally bioavailable CFTR potentiator. J Med Chem. 2014 Dec 11;57 (23) :9776-9|[4]Van Goor F, et al. 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.|[5]Mutyam V, et al. Therapeutic benefit observed with the CFTR potentiator, ivacaftor, in a CF patient homozygous for the W1282X CFTR nonsense mutation. J Cyst Fibros. 2017 Jan;16 (1) :24-29