An F508del-CFTR corrector and potentiator
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Elexacaftor

Item No. 35307

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1,3-dimethyl-1H-pyrazol-4-yl)sulfonyl]-6-[3-(3,3,3-trifluoro-2,2-dimethylpropoxy)-1H-pyrazol-1-yl]-2-[(4S)-2,2,4-trimethyl-1-pyrrolidinyl]-3-pyridinecarboxamide
CAS Number
2216712-66-0
Synonyms
  • VX-445
Molecular Formula
C26H34F3N7O4S
Formula Weight
597.7
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
279, 350 nm
SMILES
CC(C(F)(F)F)(C)COC1=NN(C2=NC(N3C(C)(C)C[C@H](C)C3)=C(C(NS(C4=CN(C)N=C4C)(=O)=O)=O)C=C2)C=C1
InChi Code
InChI=1S/C26H34F3N7O4S/c1-16-12-25(5,6)35(13-16)22-18(23(37)33-41(38,39)19-14-34(7)31-17(19)2)8-9-20(30-22)36-11-10-21(32-36)40-15-24(3,4)26(27,28)29/h8-11,14,16H,12-13,15H2,1-7H3,(H,33,37)/t16-/m0/s1
InChi Key
MVRHVFSOIWFBTE-INIZCTEOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $86

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    1 mg

    $121

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    5 mg

    $427

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    Product Description

    Elexacaftor is a corrector of the cystic fibrosis transmembrane conductance regulator (CFTR) bearing the F508 deletion (F508del) mutation, which is carried by 90% of cystic fibrosis patients, and a CFTR potentiator.1,2 It increases CFTR levels in bronchial epithelial cells isolated from patients with F508del-CFTR mutations when used at a concentration of 2 µM.1 Elexacaftor potentiates the transepithelial current in primary human nasal epithelial cells (EC50 = 1.5 nM).2 Formulations containing elexacaftor in combination with ivacaftor and tezacaftor have been used in the treatment of cystic fibrosis in patients carrying one or more mutations in the CFTR gene.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Keating, D.J., Marigowda, G., Burr, L.E., et al. VX-445–tezacaftor–ivacaftor in patients with cystic fibrosis and one or two Phe508del alleles. N. Engl. J. Med. 379(17), 1612-1620 (2018).

    2. Shaughnessy, C.A., Zeitlin, P.L., and Bratcher, P.E. Elexacaftor is a CFTR potentiator and acts synergistically with ivacaftor during acute and chronic treatment. Sci. Rep. 11(1), 19810 (2021).