VX-661

F508del CFTR corrector CAS# 1152311-62-0

VX-661

Catalog No. BCC1241----Order now to get a substantial discount!

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Chemical structure

VX-661

3D structure

Chemical Properties of VX-661

Cas No. 1152311-62-0 SDF Download SDF
PubChem ID 46199646 Appearance Powder
Formula C26H27F3N2O6 M.Wt 520.5
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Tezacaftor
Solubility DMSO : ≥ 100 mg/mL (192.12 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 1-(2,2-difluoro-1,3-benzodioxol-5-yl)-N-[1-[(2R)-2,3-dihydroxypropyl]-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)indol-5-yl]cyclopropane-1-carboxamide
SMILES CC(C)(CO)C1=CC2=CC(=C(C=C2N1CC(CO)O)F)NC(=O)C3(CC3)C4=CC5=C(C=C4)OC(O5)(F)F
Standard InChIKey MJUVRTYWUMPBTR-MRXNPFEDSA-N
Standard InChI InChI=1S/C26H27F3N2O6/c1-24(2,13-33)22-8-14-7-18(17(27)10-19(14)31(22)11-16(34)12-32)30-23(35)25(5-6-25)15-3-4-20-21(9-15)37-26(28,29)36-20/h3-4,7-10,16,32-34H,5-6,11-13H2,1-2H3,(H,30,35)/t16-/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of VX-661

DescriptionVX-661 is a second corrector of F508 del CFTR.
TargetsF508 del CFTR    

VX-661 Dilution Calculator

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VX-661 Molarity Calculator

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Preparing Stock Solutions of VX-661

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.9212 mL 9.6061 mL 19.2123 mL 38.4246 mL 48.0307 mL
5 mM 0.3842 mL 1.9212 mL 3.8425 mL 7.6849 mL 9.6061 mL
10 mM 0.1921 mL 0.9606 mL 1.9212 mL 3.8425 mL 4.8031 mL
50 mM 0.0384 mL 0.1921 mL 0.3842 mL 0.7685 mL 0.9606 mL
100 mM 0.0192 mL 0.0961 mL 0.1921 mL 0.3842 mL 0.4803 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on VX-661

VX-661, one of vertex derivatives, corrects F508del-CFTR trafficking and increases F508del-CFTR protein activity in vitro [1].

VX-661 treated alone or in combination with ivacaftor have shown to enhance F508del-CFTR trafficking to the cell surface. VX-661 has been at phase 2 study [1].

References:
[1] S. Donaldson, J. Pilewski, M. Griese, Q. Dong, P.-S. Lee, for the VX11–661-101 Study Group. WS7.3 VX-661, an investigational CFTR corrector, in combination with ivacaftor, a CFTR potentiator, in patients with CF and homozygous for the F508Del-CFTR mutation: Interim analysis. Journal of Cystic Fibrosis, Volume 12, Supplement 1, June 2013, Page S14

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References on VX-661

Novel picolinamide-based cystic fibrosis transmembrane regulator modulators: evaluation of WO2013038373, WO2013038376, WO2013038381, WO2013038386 and WO2013038390.[Pubmed:24392786]

Expert Opin Ther Pat. 2014 Jul;24(7):829-37.

Cystic fibrosis (CF) is a genetic disease caused by defects in the CF transmembrane regulator (CFTR) gene, which encodes an epithelial chloride channel. The most common mutation, Delta508CFTR, produces a protein that is misfolded and does not reach the cell membrane. The discovery that partial chloride channel function could be restored by exposure to exogenous chemical stimuli led to the search for selective CFTR modulators. Vertex has led the way in developing N-aryl-1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropanecarboxamide derivatives such as lumacaftor and VX-661, which correct trafficking of Delta508CFTR and partially restore chloride channel activity. Novartis had identified similar activity in a series of picolinamide derivatives such as 3-amino-N-[(2S)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5,6-bis(trifluoromethyl )pyridine-2-carboxamide. A series of five filings from Novartis has expanded on the activity of compounds based on this scaffold and provided compounds with nanomolar potency in cellular assays.

Some gating potentiators, including VX-770, diminish DeltaF508-CFTR functional expression.[Pubmed:25101887]

Sci Transl Med. 2014 Jul 23;6(246):246ra97.

Cystic fibrosis (CF) is caused by mutations in the CF transmembrane regulator (CFTR) that result in reduced anion conductance at the apical membrane of secretory epithelia. Treatment of CF patients carrying the G551D gating mutation with the potentiator VX-770 (ivacaftor) largely restores channel activity and has shown substantial clinical benefit. However, most CF patients carry the DeltaF508 mutation, which impairs CFTR folding, processing, function, and stability. Studies in homozygous DeltaF508 CF patients indicated little clinical benefit of monotherapy with the investigational corrector VX-809 (lumacaftor) or VX-770, whereas combination clinical trials show limited but significant improvements in lung function. We show that VX-770, as well as most other potentiators, reduces the correction efficacy of VX-809 and another investigational corrector, VX-661. To mimic the administration of VX-770 alone or in combination with VX-809, we examined its long-term effect in immortalized and primary human respiratory epithelia. VX-770 diminished the folding efficiency and the metabolic stability of DeltaF508-CFTR at the endoplasmic reticulum (ER) and post-ER compartments, respectively, causing reduced cell surface DeltaF508-CFTR density and function. VX-770-induced destabilization of DeltaF508-CFTR was influenced by second-site suppressor mutations of the folding defect and was prevented by stabilization of the nucleotide-binding domain 1 (NBD1)-NBD2 interface. The reduced correction efficiency of DeltaF508-CFTR, as well as of two other processing mutations in the presence of VX-770, suggests the need for further optimization of potentiators to maximize the clinical benefit of corrector-potentiator combination therapy in CF.

Description

Tezacaftor (VX-661) is a second F508del CFTR corrector and help CFTR protein reach the cell surface.

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