2. Membrane Transporter/Ion Channel
  3. CFTR
  4. Tezacaftor

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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CAS 番号 : 1152311-62-0

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カスタマーレビュー

Based on 25 publication(s) in Google Scholar

Other Forms of Tezacaftor:

Tezacaftor 関連抗体

Top Publications Citing Use of Products

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

    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].

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

    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.

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

    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.

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

    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.

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

    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.

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

    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.

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    製品説明

    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[1][2][3][4].

    体外実験

    Tezacaftor (2 μM, 24 h) increases the expression level of N1303K-CFTR in HEK293 and CFBE cells[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Tezacaftor 関連抗体

    Western Blot Analysis[4]

    Cell Line: HEK293, CFBE
    Concentration: 2 μM
    Incubation Time: 24 h
    Result: Increased N1303K-CFTR expression levels.
    臨床実験
    分子量

    520.50

    分子式

    C26H27F3N2O6
    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C(C1(C2=CC=C(OC(F)(F)O3)C3=C2)CC1)NC4=CC5=C(N(C[C@@H](O)CO)C(C(C)(C)CO)=C5)C=C4F
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (96.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9212 mL 9.6061 mL 19.2123 mL
    5 mM 0.3842 mL 1.9212 mL 3.8425 mL
    10 mM 0.1921 mL 0.9606 mL 1.9212 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
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    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.94%

    COA (260 KB) LCMS (97 KB)

    取扱説明書 (2659 KB)
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9212 mL 9.6061 mL 19.2123 mL 48.0307 mL
    5 mM 0.3842 mL 1.9212 mL 3.8425 mL 9.6061 mL
    10 mM 0.1921 mL 0.9606 mL 1.9212 mL 4.8031 mL
    15 mM 0.1281 mL 0.6404 mL 1.2808 mL 3.2020 mL
    20 mM 0.0961 mL 0.4803 mL 0.9606 mL 2.4015 mL
    25 mM 0.0768 mL 0.3842 mL 0.7685 mL 1.9212 mL
    30 mM 0.0640 mL 0.3202 mL 0.6404 mL 1.6010 mL
    40 mM 0.0480 mL 0.2402 mL 0.4803 mL 1.2008 mL
    50 mM 0.0384 mL 0.1921 mL 0.3842 mL 0.9606 mL
    60 mM 0.0320 mL 0.1601 mL 0.3202 mL 0.8005 mL
    80 mM 0.0240 mL 0.1201 mL 0.2402 mL 0.6004 mL
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    Tezacaftor Related Classifications

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    一般には略語で表示されます：C1V1 = C2V2

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Tezacaftor1152311-62-0VX-661VX661VX 661CFTRCystic fibrosis transmembrane conductance regulatorModulatorHEK293CFBELung transplantationInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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