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Tezacaftor

(別名: VX-661)
31 Cited Publications
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Based on 31 publication(s) in Google Scholar

Tezacaftor (VX-661) is a F508del CFTR corrector. It helps CFTR protein reach the cell surface. However, Ivacaftor (VX-770, HY-13017), a CFTR potentiator, helps to prolong the opening time of cell surface CFTR protein channels. Tezacaftor combining with Ivacaftor, shows potent efficacy against cystic fibrosis and diseases with homozygous for the CFTR Phe508del mutation. Moreover, Elexacaftor (VX-445, HY-111772) is also a CFTR corrector. Elexacaftor-Tezacaftor-Ivacaftor aims at with cystic fibrosis (CF) with at least one Phe508del mutation, often avoids the indication for lung transplantation.

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  • 純度 : 99.85%
  • CAS 番号: 1152311-62-0
  • 分子式: C26H27F3N2O6
  • 分子量:520.50
  • 保管条件:

    4°C, stored under nitrogen

    * In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

  • Tezacaftor Chemical Structure
    Tezacaftor 構造式
  • Experimental Validation Results for Tezacaftor
  • Experimental Validation Results for Tezacaftor
  • Experimental Validation Results for Tezacaftor
  • Experimental Validation Results for Tezacaftor
  • Experimental Validation Results for Tezacaftor
  • Experimental Validation Results for Tezacaftor
CAS 番号: 1152311-62-0
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WB2D/3D Cell Culture and DifferentiationBio/Physico-chemical Assay
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  • Bio/Physico-chemical Assay
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  • Tezacaftor Chemical Structure
    Tezacaftor Chemical Structure
    1/16
  • 1/16

    Tezacaftor purchased from MedChemExpress. Usage Cited in: J Med Chem. 2025 Feb 27;68(4):4596-4618. [Abstract]

    Customer Validation
     ARN23765 stabilizes NBD1-ICL4 and NBD1-ICL1 interactions. HEK293 cells were transfected with the constructs coding for F508del-CFTR, F508del/R1070W-CFTR, and R170G-CFTR and incubated for 24 h with ARN23765 (10 nM) or Tezacaftor (VX-661, 3 μM). DMSO (0.2%) was used as negative control. Left: representative WBs with detection of CFTR B- and C-bands. Right: quantification (mean ± SD, 3–4 independent experiments) of CFTR band-C abundance, calculated using the conventional equation [band-C/band C+B].

  • 1/16

    Tezacaftor purchased from MedChemExpress. Usage Cited in: J Med Chem. 2025 Feb 27;68(4):4596-4618. [Abstract]

    Customer Validation
     ARN23765 stabilizes NBD1-ICL4 and NBD1-ICL1 interactions. HEK293 cells were transfected with the constructs coding for F508del-CFTR, F508del/R1070W-CFTR, and R170G-CFTR and incubated for 24 h with ARN23765 (10 nM) or Tezacaftor (VX-661, 3 μM). DMSO (0.2%) was used as negative control. CFTR channel activity was evaluated with fluorometric imaging plate reader functional assay (FLIPR).40 Plasma membrane depolarization was detected as an increase in fluorescence (ΔF), after which CFTR was inhibited by the addition of inhibitor-172, (10 μM). Left: representative fluorescence traces. Right: peak change in fluorescence (mean ± SD, 8 replicates), expressed relative to baseline fluorescence (ΔF/F0). FSK: forskolin; CFTR Inh: inhibitor-172.

  • 1/16

    Tezacaftor purchased from MedChemExpress. Usage Cited in: iScience. 2024 Aug 9;27(9):110703. [Abstract]

    Customer Validation
     Representative traces of whole-cell currents of HEK-293 cells cotransfected with PIEZO1 and CFTR mutant F508del, pre-treated with combination of CFTR correctors VX445/VX661 (Tezacafto) (2 μM each) for 24 h.107 Bath solution contained 10 μM Yoda1, 20 μM Forskolin, and 20 μM CFTRinh-172.

  • 1/16

    Tezacaftor purchased from MedChemExpress. Usage Cited in: iScience. 2024 Aug 9;27(9):110703. [Abstract]

    Customer Validation
     Summary of Yoda1-induced current in HEK-293 cells transfected with PIEZO1 only or cotransfected with PIEZO1 and CFTR mutant F508del. Cells were pre-treated with or without combination of CFTR correctors VX445/VX661 (Tezacafto) (2 μM each) for 24 h.

  • 1/16

    Tezacaftor purchased from MedChemExpress. Usage Cited in: Cell. 2022 Jan 6;185(1):158-168.e11. [Abstract]

    Customer Validation
     Competition binding assay. The binding of [H3]lumacaftor (10 nM) was plotted as a function of the competitor’s concentration. Data were fit to a single-site competitive binding model. The Ki values for lumacaftor and Tezacaftor are 7.7 ± 2.0 nM and 0.12 ± 0.04 mM, respectively. No competition was observed for elexacaftor and Corr-4a.

  • 1/16

    Tezacaftor purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2020 Dec 31;22(1):344. [Abstract]

    Customer Validation
     Representative brightfield images of G542X intestinal organoids treated with 100 µM G418, 2.5 mM gentamicin, or 2.5 mM paromomycin and indicated combinations of 1 µM SMG1i and/or 3.3 µM Tezacaftor (VX-661) at 0 min and 180 min following treatment with 10 µM forskolin. Scale bar is 100 µm.

  • Tezacaftor