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    Tezacaftor (VX-661)
    Tezacaftor (VX-661)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1691
    CAS #: 1152311-62-0Purity ≥98%

    Description: Tezacaftor (formerly VX-661; trade name: Symdeko) is a second F508del CFTR corrector that is able to help CFTR protein reach the cell surface. VX-661 is potentially useful for treatment of cystic fibrosis disease. In Feb 2018, Tezacaftor was approved by FDA to treat cystic fibrosis in patients age 12 years and older. Cystic fibrosis (CF) is a genetic disease caused by defects in the CF transmembrane regulator (CFTR) gene, which encodes an epithelial chloride channel. The most common mutation, Δ508CFTR, produces a protein that is misfolded and does not reach the cell membrane. VX-661 can correct trafficking of Δ508CFTR and partially restore chloride channel activity. 

    References: Sci Transl Med. 2014 Jul 23;6(246):246ra97.

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    Molecular Weight (MW)520.5
    CAS No.1152311-62-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (192.1 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILESO=C(C1(C2=CC=C(OC(F)(F)O3)C3=C2)CC1)NC4=CC5=C(N(C[[email protected]@H](O)CO)C(C(C)(C)CO)=C5)C=C4F
    SynonymsVX-661; VX661; VX 661; Trikafta.

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    In Vitro

    In vitro activity: VX-661, known as a CTFR corrector, allows F508del mutant channels to escape degradation and transit to the cell membrane.

    Kinase Assay: In vitro, a combination of VX-661 and ivacaftor results in greater CFTR activity compared with VX-661 alone.

    Cell Assay: VX-661 treated alone or in combination with ivacaftor have shown to enhance F508del-CFTR trafficking to the cell surface. VX-661 has been at phase 2 study

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    ReferencesSci Transl Med. 2014 Jul 23;6(246):246ra97.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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