A F508del-CFTR corrector
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VX-809

Item No. 22196

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[6-[[[1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl]amino]-3-methyl-2-pyridinyl]-benzoic acid
CAS Number
936727-05-8
Synonyms
  • Lumacaftor
  • VRT-826809
Molecular Formula
C24H18F2N2O5
Formula Weight
452.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/mlEthanol: 25 mg/ml
λmax
217, 291 nm
SMILES
OC(C1=CC(C2=C(C)C=CC(NC(C3(CC3)C4=CC(OC(F)(F)O5)=C5C=C4)=O)=N2)=CC=C1)=O
InChi Code
InChI=1S/C24H18F2N2O5/c1-13-5-8-19(27-20(13)14-3-2-4-15(11-14)21(29)30)28-22(31)23(9-10-23)16-6-7-17-18(12-16)33-24(25,26)32-17/h2-8,11-12H,9-10H2,1H3,(H,29,30)(H,27,28,31)
InChi Key
UFSKUSARDNFIRC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $167

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    10 mg

    $293

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    25 mg

    $631

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    Product Description

    VX-809 is a small molecule that corrects the processing of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing the F508 deletion (F508del) mutation carried by 90% of cystic fibrosis patients.1 It enhances F508del-CFTR protein maturation and restores chloride transport function in FRT cells (EC50s = 100 and 500 nM, respectively). VX-809 increases the amount of F508del-CFTR protein exiting the endoplasmic reticulum in HEK293 cells expressing the mutant receptor. It also increases chloride and fluid transport in cultured human bronchial epithelial cells isolated from cystic fibrosis patients carrying the F508del-CFTR mutation. Formulations containing VX-809 are being investigated clinically for the treatment of cystic fibrosis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Van Goor, F., Hadida, S., Grootenhuis, P.D., et al. Correction of the F508del-CFTR protein processing defect in vitro by the investigational drug VX-809. Proc. Natl. Acad. Sci. USA 108(46), 18843-18848 (2011).