Molecular Weight(MW): 520.5
Tezacaftor (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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(B)ΔISC response to forskolin observed in VX-661-treated CF HBE cells (*P = 0.0021, VX661 vs. vehicle) was prevented by chronic VX-770 treatment and significantly different from VX-661-treated cells (#P=0.0126, VX661 vs. VX661+VX770). (C) The response to CFTR inh-172 that was observed in VX-661-treated cells (*P = 0.0111, VX661 vs. vehicle) was significantly decreased in VX809+VX770 treated cells (#P = 0.0038, VX661 vs. VX661+VX770). Primary CF HBE cultures (ΔF508/ΔF508) were derived from 3 different patients, and 3-4 replicates were performed per patient.
Sci Transl Med 2014 6(246), 246ra96. Tezacaftor (VX-661) purchased from Selleck.
Bar graphs represent maximum percentage change in fluorescence (ΔF) after addition of CFTR agonist, relative to baseline (F0) measurements prior to agonist addition (time = 10 min). Asterisks indicate statistical significance using one-way ANOVA and Tukey’s multiple comparison tests for the three distinct differentiations (*p < 0.05, **p < 0.01, ***p < 0.001).
NPJ Genom Med. 2017, 2:12. Tezacaftor (VX-661) purchased from Selleck.
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|Description||Tezacaftor (VX-661) is a second F508del CFTR corrector and is believed to help CFTR protein reach the cell surface. Phase 2.|
VX-661, known as a CTFR corrector, allows F508del mutant channels to escape degradation and transit to the cell membrane.
|In vitro||DMSO||100 mg/mL (192.12 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02953314||Completed||Drug: VX-661|Drug: Ivacaftor||Cystic Fibrosis||Vertex Pharmaceuticals Incorporated||October 2016||Phase 3|
|NCT02565914||Enrolling by invitation||Drug: VX-661/ivacaftor|Drug: ivacaftor||Cystic Fibrosis||Vertex Pharmaceuticals Incorporated||August 2015||Phase 3|
|NCT02412111||Completed||Drug: Ivacaftor|Drug: Tezacaftor/Ivacaftor||Cystic Fibrosis||Vertex Pharmaceuticals Incorporated||June 2015||Phase 3|
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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