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Lumacaftor

Catalog No. T2595 CAS 936727-05-8

Synonyms: VX-809, VRT 826809

Lumacaftor (VRT 826809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein. It enhances F508del-CFTR protein maturation in FRT cells (EC50: 100 nM).

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Lumacaftor, CAS 936727-05-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 61.00
25 mg	In stock	$ 75.00
50 mg	In stock	$ 98.00
100 mg	In stock	$ 125.00
500 mg	In stock	$ 313.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.72%

Purity: 99.68%

Biological Description

Chemical Properties

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Description	Lumacaftor (VRT 826809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein. It enhances F508del-CFTR protein maturation in FRT cells (EC50: 100 nM).
Targets&IC50	F508del CFTR:0.1 μM (EC50, Fischer rat thyroid cells)
In vitro	In cultured human bronchial epithelial cells isolated from patients with CF homozygous for F508del, Lumacaftor (VX-809) improved F508del-CFTR processing in the endoplasmic reticulum and enhanced chloride secretion to approximately 14% of non-CF human bronchial epithelial cells (EC50: 81 nM), a level associated with mild CF in patients with less disruptive CFTR mutations [1]. VX-809 produced a concentration-dependent increase in the HRP luminescence signal after incubation with cells at 37°C or 27°C in both cell lines, with a similar EC50 value of approximately 0.3 μM [2].
Kinase Assay	In one set of assays, R1070W-?F508-CFTR-HRP (R1070W-HRP)–expressing CFBE41o? cells were incubated with 100 μl medium containing 25 μM test compounds and 0.5 μg/ml doxycycline for 24 hours at 37°C. In a second set of assays, ?F508-CFTR-HRP (?F508-HRP)–expressing CFBE41o? cells were incubated with 100 μl medium containing 25 μM test compounds, 2 μM VX-809, and 0.5 μg/ml doxycycline for 24 hours at 37°C. All compound plates contained negative controls (DMSO vehicle) and positive controls [2 μM VX-809]. In both assays, the cells were washed four times with PBS, and HRP activity was assayed by the addition of 50 μl/well of HRP substrate. After shaking for 5 minutes, chemiluminescence was measured using a Tecan Infinite M1000 plate reader (Tecan Groups Ltd, Mannedorf, Switzerland) equipped with an automated stacker (integration time, 100 milliseconds). Z′ is defined as = 1 ? [(3 × standard deviation of maximum signal control + 3 × standard deviation of minimum signal control)/absolute (mean of maximum signal control ? mean of minimum signal control)] [2].
Cell Research	FRT, HEK-293, or HBE cells expressing CFTR or F508del-CFTR were incubated for 24 h at 37 °C with or without VX-809 in the assay media. After incubation, cells were harvested in ice-cold D-PBS solution (without calcium and magnesium) and pelleted at 1,000 × g at 4 °C. Cell pellets were lysed in 1% Nonidet P-40, 0.5% sodium deoxycholate, 200 mM NaCl, 10 mM Tris, pH 7.8, and 1 mM EDTA plus protease inhibitor mixture (1:250) for 30 min on ice. Lysates were spun for 10 min at 10,000 × g at 4 °C to pellet nuclei and insoluble material. Approximately 12 μg total protein was heated in Laemmli buffer with 5% β-mercaptoethanol at 37 °C for 5 min and loaded onto a 3% to 8% Tris-acetate gel. The gel was transferred to nitrocellulose and processed for Western blotting by using monoclonal CFTR antibody 769 or polyclonal to GAPDH. Blots were developed by enhanced chemiluminescence. Quantification of the relative amounts of bands C and GAPDH was performed by using NIH ImageJ analysis of scanned films [1].

Synonyms	VX-809, VRT 826809
Molecular Weight	452.41
Formula	C24H18F2N2O5
CAS No.	936727-05-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 6 mg/mL (13.26 mM)

DMSO: 83 mg/mL (183.5 mM)

References and Literature

1. Van Goor F, et al. Correction of the F508del-CFTR protein processing defect in vitro by the investigational drug VX-809. Proc Natl Acad Sci U S A. 2011 Nov 15;108(46):18843-8. 2. Phuan PW, et al. Synergy-based small-molecule screen using a human lung epithelial cell line yields ΔF508-CFTR correctors that augment VX-809 maximal efficacy. Mol Pharmacol. 2014 Jul;86(1):42-51.

Citations

1. Sondo E, Cresta F, Pastorino C, et al. The L467F-F508del Complex Allele Hampers Pharmacological Rescue of Mutant CFTR by Elexacaftor/Tezacaftor/Ivacaftor in Cystic Fibrosis Patients: The Value of the Ex Vivo Nasal Epithelial Model to Address Non-Responders to CFTR-Modulating Drugs. International Journal of Molecular Sciences. 2022, 23(6): 3175. 2. Baldassarri M, Zguro K, Tomati V, et al.Gain-and Loss-of-Function CFTR Alleles Are Associated with COVID-19 Clinical Outcomes.Cells.2022, 11(24): 4096. 3. Tomati V, Costa S, Capurro V, et al.Rescue by elexacaftor-tezacaftor-ivacaftor of the G1244E cystic fibrosis mutation's stability and gating defects are dependent on cell background.Journal of Cystic Fibrosis.2022

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library EMA Approved Drug Library Drug Repurposing Compound Library Anti-Cancer Drug Library FDA-Approved Drug Library Anti-Fibrosis Compound Library Anti-Cancer Compound Library Clinical Compound Library Bioactive Compound Library

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Keywords

Lumacaftor 936727-05-8 Autophagy Membrane transporter/Ion channel CFTR VX 809 VX809 VX-809 Cystic fibrosis transmembrane conductance regulator VRT826809 Inhibitor VRT-826809 inhibit VRT 826809 inhibitor

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