Tezacaftor (VX-661)

Catalog No.S7059 Batch:S705903

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Technical Data

Formula

C26H27F3N2O6
Molecular Weight 520.5 CAS No. 1152311-62-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (192.12 mM)
Ethanol 100 mg/mL (192.12 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Tezacaftor (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.

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    Primary HBE cells

  • Concentrations

    5 μM

  • Incubation Time

    24 h

  • Method

    Cells were treated with indicated concentration of drug for 24 h.
Animal Study:

[3]
  • Animal Models

    Male FVB/n mice

  • Dosages

    2 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by Sci Transl Med, 2014, 6(246), 246ra96]

Data from [Data independently produced by , , J Cyst Fibros, 2018, doi:10.1016/j.jcf.2018.07.001]

Data from [Data independently produced by , , NPJ Genom Med. 2017, 2:12]

Selleck's Tezacaftor (VX-661) has been cited by 105 publications

PTI-801 (posenacaftor) shares a common mechanism with VX-445 (elexacaftor) to rescue p.Phe508del-CFTR [ Eur J Pharmacol, 2024, 967:176390] PubMed: 38336013
CFTR function is impaired in a subset of patients with pancreatitis carrying rare CFTR variants [ Pancreatology, 2024, S1424-3903(24)00066-8] PubMed: 38493004
A uniquely efficacious type of CFTR corrector with complementary mode of action [ Sci Adv, 2024, 10(9):eadk1814] PubMed: 38427726
UBE3C Facilitates the ER-Associated and Peripheral Degradation of Misfolded CFTR [ Cells, 2023, 12(23)2741] PubMed: 38067172
A Novel Co-Culture Model Reveals Enhanced CFTR Rescue in Primary Cystic Fibrosis Airway Epithelial Cultures with Persistent Pseudomonas aeruginosa Infection [ Cells, 2023, 10.3390/cells12222618] PubMed: 37998353
Putting bicarbonate on the spot: pharmacological insights for CFTR correction in the airway epithelium [ Front Pharmacol, 2023, 14:1293578] PubMed: 38149052
Elexacaftor Mediates the Rescue of F508del CFTR Functional Expression Interacting with MSD2 [ Int J Mol Sci, 2023, 24(16)12838] PubMed: 37629017
Theratyping of the Rare CFTR Genotype A559T in Rectal Organoids and Nasal Cells Reveals a Relevant Response to Elexacaftor (VX-445) and Tezacaftor (VX-661) Combination [ Int J Mol Sci, 2023, 24(12)10358] PubMed: 37373505
CFTR Function Restoration upon Elexacaftor/Tezacaftor/Ivacaftor Treatment in Patient-Derived Intestinal Organoids with Rare CFTR Genotypes [ Int J Mol Sci, 2023, 24(19)14539] PubMed: 37833986
Rescue of Rare CFTR Trafficking Mutants Highlights a Structural Location-Dependent Pattern for Correction [ Int J Mol Sci, 2023, 24(4)3211] PubMed: 36834620

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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