VX-661 is a second F508del CFTR corrector and is believed to help CFTR protein reach the cell surface. Phase 2.

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VX-661 Chemical Structure

VX-661 Chemical Structure
Molecular Weight: 520.5

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Product Information

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  • Research Area
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    Combination Therapy

Product Description

Biological Activity

Description VX-661 is a second F508del CFTR corrector and is believed to help CFTR protein reach the cell surface. Phase 2.
Targets F508del-CFTR [1]
(Cell-free assay)
In vitro VX-661, known as a CTFR corrector, allows F508del mutant channels to escape degradation and transit to the cell membrane.
In vivo

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Vertex to host investor conference

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-11-14)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02565914 Recruiting Cystic Fibrosis Vertex Pharmaceuticals Incorporated August 2015 Phase 3
NCT02516410 Recruiting Cystic Fibrosis Vertex Pharmaceuticals Incorporated August 2015 Phase 3
NCT02508207 Not yet recruiting Cystic Fibrosis Vertex Pharmaceuticals Incorporated August 2015 Phase 2
NCT02412111 Recruiting Cystic Fibrosis Vertex Pharmaceuticals Incorporated May 2015 Phase 3
NCT02392234 Recruiting Cystic Fibrosis Vertex Pharmaceuticals Incorporated March 2015 Phase 3

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Chemical Information

Molecular Weight (MW) 520.5


CAS No. 1152311-62-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 100 mg/mL (192.12 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Cyclopropanecarboxamide, 1-(2,2-difluoro-1,3-benzodioxol-5-yl)-N-[1-[(2R)-2,3-dihydroxypropyl]-6-fluoro-2-(2-hydroxy-1,1-dimethylethyl)-1H-indol-5-yl]-

Customer Product Validation (1)

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Source Sci Transl Med 2014 6(246), 246ra96. VX-661 purchased from Selleck
Method ISC measurements in Ussing chambers
Cell Lines CF HBE cells
Incubation Time 48 h
Results In contrast, rescue of ΔISC CFTR function was markedly increased in cultures that had been chronically treated with VX-661 and VX-770 compared to VX-661 alone. It also tested the impact of chronic VX-770 treatment on ΔF508 correction in CF HBE cultures (ΔF508/ΔF508) by the corrector compound VX-661. Similar to VX-809-treated CF cells, VX-661-corrected CF HBE cells showed a drastic reduction in forskolin-mediated CFTR function when VX-770 was chronically added.

Product Use Citation (1)

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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