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Chemical Structure : Lumacaftor
CAS No.: 936727-05-8
Catalog No.: PC-43442Not For Human Use, Lab Use Only.
VX-809 (Lumacaftor, VRT 826809) is a potent CFTR corrector that increases F508del-CFTR-mediated chloride transport amd improves F508del-CFTR maturation in FRT cells with EC50 of 0.1 and 0.5 uM, respectively, also inhibits dual specificity phosphatase 18 (DUSP18).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $88 | In stock | |
| 50 mg | $158 | In stock | |
| 100 mg | $218 | In stock | |
| 250 mg | Get quote | ||
| 1 g | Get quote |
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VX-809 (Lumacaftor, VRT 826809) is a potent CFTR corrector that increases F508del-CFTR-mediated chloride transport amd improves F508del-CFTR maturation in FRT cells with EC50 of 0.1 and 0.5 uM, respectively, also inhibits dual specificity phosphatase 18 (DUSP18).
VX-809 (Lumacaftor, VRT 826809) improves F508del-CFTR processing in the endoplasmic reticulum and enhances chloride secretion to approximately 14% of non-CF human bronchial epithelial cells (EC50=81 nM).
VX-809 (Lumacaftor, VRT 826809) exhibits biochemical and functional characteristics similar to normal CFTR, including biochemical susceptibility to proteolysis, residence time in the plasma membrane, and single-channel open probability after F508del-CFTR corrected by VX-809.
VX-809 (Lumacaftor, VRT 826809) inhibits CRC growth in mice and synergistically enhances anti-tumor immunity when combined with an anti-PD-1 antibody.
| M.Wt | 452.41 | |
| Formula | C24H18F2N2O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Benzoic acid, 3-[6-[[[1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl]amino]-3-methyl-2-pyridinyl]- |
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1. Van Goor F, et al. Proc Natl Acad Sci U S A. 2011 Nov 15;108(46):18843-8.
2. Okiyoneda T, et al. Nat Chem Biol. 2013 Jul;9(7):444-54.
3. Farinha CM, et al. Chem Biol. 2013 Jul 25;20(7):943-55.
4. Kopeikin Z, et al. J Cyst Fibros. 2014 Sep;13(5):508-14.
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