Tezacaftor (VX-661)

Catalog No.S7059 Batch:S705904

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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 13 mg/mL (24.97 mM)
Water Insoluble
* <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.)

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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 121 publications

Septin-dependent defense mechanisms against Pseudomonas aeruginosa are stalled in cystic fibrosis bronchial epithelial cells [ Eur J Cell Biol, 2024, 103(2):151416] PubMed: 38636185
Ligand-based virtual-screening identified a novel CFTR ligand which improves the defective cell surface expression of misfolded ABC transporters [ Front Pharmacol, 2024, 15:1370676] PubMed: 38666024
Comprehensive Assessment of CFTR Modulators' Therapeutic Efficiency for N1303K Variant [ Int J Mol Sci, 2024, 25(5)2770] PubMed: 38474016
Estimation of Chloride Channel Residual Function and Assessment of Targeted Drugs Efficiency in the Presence of a Complex Allele [L467F;F508del] in the CFTR Gene [ Int J Mol Sci, 2024, 25(19)10424] PubMed: 39408749
PTI-801 (posenacaftor) shares a common mechanism with VX-445 (elexacaftor) to rescue p.Phe508del-CFTR [ Eur J Pharmacol, 2024, 967:176390] PubMed: 38336013
Localization and function of humanized F508del-CFTR in mouse intestine following activation of serum glucocorticoid kinase 1 and Trikafta [ Eur J Pharmacol, 2024, 978:176771] PubMed: 38925289
Reduced sialylation of airway mucin impairs mucus transport by altering the biophysical properties of mucin [ Sci Rep, 2024, 14(1):16568] PubMed: 39019950
CFTR modulators response of S737F and T465N CFTR variants on patient-derived rectal organoids [ Orphanet J Rare Dis, 2024, 19(1):343] PubMed: 39272186
CFTR function is impaired in a subset of patients with pancreatitis carrying rare CFTR variants [ Pancreatology, 2024, S1424-3903(24)00066-8] PubMed: 38493004
Functional rescue of CFTR in rectal organoids from patients carrying R334W variant by CFTR modulators and PDE4 inhibitor Roflumilast [ Respir Investig, 2024, 62(3):455-461] PubMed: 38547757

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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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