VX-770 Inhibitor CAS No. 873054-44-5

Cat. No.	Name	Size	Price
KI0152	VX-770	5 mg	$272
	VX-770	10 mg	$320
	VX-770	50 mg	$1552
	VX-770	200 mg	$3952

Chemical Characteristic

Product Name	VX-770
Synonyms	Ivacaftor, Kalydeco
CAS No.	873054-44-5
Molecular Weight	392.49
Formula	C₂₄H₂₈N₂O₃
Chemical Name	N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide
Smiles	[nH]1cc(c(=O)c2ccccc12)C(=O)Nc1c(cc(c(c1)O)C(C)(C)C)C(C)(C)C
Chemical Structure

Biological activities

VX-770 is a potentiator of cystic fibrosis transmembrane conductance regulator (CFTR) targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM, respectively. In the recombinant Fisher rat thyroid (FRT) cells expressing G551D gating mutation of CFTR, VX-770 (10µM) increases the forskolin-stimulated transepithelial current (IT) by 4-fold with an EC50 of 100 nM and this response is blocked by the CFTR inhibitor CFTRinh-172. In the recombinant FRT cells expressing temperature-corrected F508del processing mutation of CFTR, VX-770 (10µM) increases the forskolin-stimulated IT by about 6-fold with an EC50 of 25 nM and this response is also blocked by the CFTR inhibitor CFTRinh-172. In excised membrane patches from recombinant cells expressing G551D-, F508del-, or wild-type CFTR, VX-770 (10µM) increases the open probability (Po) of G551D-, F508del- and wild-type CFTR by 6-fold, 5-fold and 2-fold, respectively. In human bronchial epithelia (HBE) isolated from the bronchi of a single CF donor lung carrying the G551D and F508del CFTR mutations, VX-770 increases the forskolin-stimulated IT with an EC50 of 236 nM. VX-770 is about 70-fold more potent than the commonly used CFTR potentiator genistein. VX-770 (10µM) increases the forskolin-stimulated IT in G551D/F508del HBE by about10-fold from 5% to 48% of that measured in non-CF HBE. Furthermore, VX-770 (10µM) causes a significant increase in the forskolin-stimulated IT in F508del HBE isolated from three of the six individuals with a mean EC50 of 22 nM and a maximum response of 16% non-CF HBE. The magnitude of the effect on the forskolin-stimulated IT in F508del HBE is less than in G551D/F508del HBE. VX-770 (10µM) decreases the potential difference (PD) with an IC50 of 43 nM and decreases the amiloride response in G551D/F508del HBE.^[1] Besides, acute (5 minutes) addition of 10µM VX-770 increases the channel Po of all CFTR gating mutations tested (G551D-, G178R-, S549N-, S549R-, G551S-, G970R-, G1244E-, S1251N-, S1255P-, and G1349D-CFTR), reaching levels equivalent to 30% to 118% of normal CFTR in FRT cells.^[2]

References

[1] 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, 106(44): 18825-18830. [2] Yu H, et al. Ivacaftor potentiation of multiple CFTR channels with gating mutations. J Cyst Fibros. 2012, 11(3): 237-245 .

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