VX-809 Inhibitor CAS No. 936727-05-8

Cat. No.	Name	Size	Price
KI1338	VX-809	5 mg	$272
	VX-809	10 mg	$512
	VX-809	50 mg	$1552
	VX-809	200 mg	$3952

Chemical Characteristic

Product Name	VX-809
CAS No.	936727-05-8
Molecular Weight	452.41
Formula	C₂₄H₁₈F₂N₂O₅
Chemical Name	3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
Smiles	C(=O)(c1cc(ccc1)c1c(ccc(n1)NC(=O)C1(CC1)c1cc2OC(Oc2cc1)(F)F)C)O
Chemical Structure

Biological activities

VX-809 is a cystic fibrosis transmembrane conductance regulator (CFTR) modulator. VX-809 is used to treat cystic fibrosis. VX-809 improves CFTR function in at least one organ (sweat gland). VX-809 reduces elevated sweat chloride values in a dose-dependent manner. ^[1] In cultured human bronchial epithelial cells, VX-809 improves F508del-CFTR processing in the endoplasmic reticulum and enhances chloride secretion to approximately 14% of non-CF human bronchial epithelial cells with an EC50 of 81 nM. F508del-CFTR corrected by VX-809 reveals biochemical and functional characteristics similar to normal CFTR, including biochemical susceptibility to proteolysis, residence time in the plasma membrane, and single-channel open probability. VX-809 enhances F508del-CFTR maturation and chloride transport in FRT cells. In FRT cells, VX-809 improves F508del-CFTR maturation by 7.1 fold compared with vehicle-treated cells. At VX-809 concentrations greater than 10 µM, the response is reduced, resulting in a bell-shaped dose??esponse relationship with an IC50 of approximately 100 µM. VX-809 enhances chloride and fluid transport in cultures of CF airway epithelial cells.^[2]

Protocols

In vitro: VX-809 is dissolved in DMSO.^[2]

References

[1] Clancy JP, et al. Results of a phase IIa study of VX-809, an investigational CFTR corrector compound, in subjects with cystic fibrosis homozygous for the F508del-CFTR mutation.Thorax. 2012, 67(1): 12-18. [2] Van Goor F, et al. Correction of the F508del-CFTR protein processing defect in vitro by the investigational drug VX-809. Proc Natl Acad Sci USA. 2011, 108(46): 18843-18848.

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