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Lumacaftor (VX-809)
Catalog No.S1565 Synonyms: VRT 826809
For research use only.
Lumacaftor (VX-809, VRT 826809) acts to correct CFTR mutations common in cystic fibrosis by increasing mutant CFTR (F508del-CFTR) maturation,EC50 of 0.1 μM in fisher rat thyroid cells. Phase 3.
CAS No. 936727-05-8
Selleck's Lumacaftor (VX-809) has been cited by 188 publications
Purity & Quality Control
Choose Selective CFTR Inhibitors
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Biological Activity
| Description | Lumacaftor (VX-809, VRT 826809) acts to correct CFTR mutations common in cystic fibrosis by increasing mutant CFTR (F508del-CFTR) maturation,EC50 of 0.1 μM in fisher rat thyroid cells. Phase 3. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Features | Higher specificity and efficacy relative to other CFTR defect drugs. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Targets |
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| In vitro |
VX-809 acts at the level of the ER to allow a fraction of the F508del-CFTR to adopt a properly folded form, to exit the ER and mobilize to the cell surface for normal functioning. In Fischer rat thyroid (FRT) cells expressing F508del-CFTR, VX-809 treatment significantly improves F508del-CFTR maturation by 7.1 fold with an EC50 of 0.1 μM, and enhances F508del-CFTR-mediated chloride transport by approximately 5 fold with EC50 of 0.5 μM, while VRT-768 has higher EC50 values of 7.9 μM and 16 μM, respectively. In HEK-293 cells expressing F508del-CFTR, VX-809 (3 μM) treatment increases F508del-CFTR exit from the ER by 6 fold, reaching levels comparable to 34% of CFTR. In primary human bronchial epithelial (HBE) cells with F508del-CFTR mutation, VX-809 increases CFTR maturation and enhances chloride secretion with EC50 of 350 nM and 81 nM, respectively, more efficacious than Corr-4a and VRT-325. F508del-CFTR corrected by VX-809 exhibits single-channel open probability of 0.39 similar to normal CFTR of 0.40. Unlike VX-770, VX-809 is not a CFTR potentiator, as acute addition of VX-809 has no effect on F508del-CFTR function. In contrast to VRT-325 and Corr-4a, VX-809 does not improve the processing of the normal or mutant forms of hERG or P-gp, as well as other disease-causing mislocalized proteins, including α1-antitrypsin Z mutant (E342K-α1-AT) or N370S-β-glucosidase, suggesting that VX-809 is specific for CFTR. VX-809 in combination with VRT-325 or Corr-4a has additive effect on CFTR-mediated chloride transport in cultured F508del-HBE. [1] |
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| Cell Data |
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| Assay |
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Protocol (from reference)
| Kinase Assay:[1] |
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|---|---|
| Cell Research:[1] |
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Solubility (25°C)
|
In vitro |
DMSO |
90 mg/mL
(198.93 mM) |
| Water |
Insoluble
|
|
| Ethanol |
'6 mg/mL
|
|
|
In vivo |
Add solvents to the product individually and in order |
30 mg/mL |
Chemical Information
| Molecular Weight | 452.41 | ||
|---|---|---|---|
| Formula | C24H18F2N2O5 |
||
| CAS No. | 936727-05-8 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CC1=C(N=C(C=C1)NC(=O)C2(CC2)C3=CC4=C(C=C3)OC(O4)(F)F)C5=CC(=CC=C5)C(=O)O | ||
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT03512119 | Completed | Drug: Lumacaftor-Ivacaftor treatment | Cystic Fibrosis Homozygous for Phe 508 Del CFTR|Glucose Intolerance or Newly Diagnosis Diabetes | University Hospital Strasbourg France | February 11 2016 | -- |
| NCT02589236 | Completed | Drug: Cavosonstat|Drug: Placebo | Cystic Fibrosis | Nivalis Therapeutics Inc.|Medidata Solutions | November 2015 | Phase 2 |
| NCT02514473 | Completed | Drug: VX-809|Drug: Placebo|Drug: VX-770 | Cystic Fibrosis | Vertex Pharmaceuticals Incorporated | July 2015 | Phase 3 |
| NCT01899105 | Completed | Drug: lumacaftor|Drug: ivacaftor | Cystic Fibrosis | Vertex Pharmaceuticals Incorporated | July 2013 | Phase 1 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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