Elexacaftor (VX-445)

Catalog No.S8851 Batch:S885101

Technical Data

Formula

C₂₆H₃₄F₃N₇O₄S

Molecular Weight

597.65

CAS No.

2216712-66-0

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (167.32 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 95% Corn oil	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/mL clarified DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2.5mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween-80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O Dilute to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Elexacaftor (VX-445) is a next-generation cystic fibrosis transmembrane conductance regulator (CFTR) corrector.This is a compound which is not chiral purity.

Targets

CFTR ^[1]

In vitro

The pendrin-dependent increase in cystic fibrosis transmembrane conductance regulator (CFTR) current is additive with the CFTR modulator elexacaftor.^[2]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines Human bronchial epithelial cells from DeltaF508/DeltaF508 Cystic Fibrosis patients (CF HBECs) Concentrations 3 µM Incubation Time 48 h Method Using Chamber recordings from DeltaF508/DeltaF508 CF HBEC epithelia were treated with the LIE triple combination for 48 h plus and minus 10 ng/mL IL-13 and/or 10 micromol/L niflumic acid (for 30 minutes) again. Transepithelial current (Isc) and conductance (Gt) were measured. (Data sourced from selleck products)

Cell Assay:^{^[2]}

Cell lines
Human bronchial epithelial cells from DeltaF508/DeltaF508 Cystic Fibrosis patients (CF HBECs)
Concentrations
3 µM
Incubation Time
48 h
Method
Using Chamber recordings from DeltaF508/DeltaF508 CF HBEC epithelia were treated with the LIE triple combination for 48 h plus and minus 10 ng/mL IL-13 and/or 10 micromol/L niflumic acid (for 30 minutes) again. Transepithelial current (Isc) and conductance (Gt) were measured.

(Data sourced from selleck products)

References

Selleck's Elexacaftor (VX-445) has been cited by 64 publications

Septin-dependent defense mechanisms against Pseudomonas aeruginosa are stalled in cystic fibrosis bronchial epithelial cells [ Eur J Cell Biol, 2024, 103(2):151416]	PubMed: 38636185
Ligand-based virtual-screening identified a novel CFTR ligand which improves the defective cell surface expression of misfolded ABC transporters [ Front Pharmacol, 2024, 15:1370676]	PubMed: 38666024
Comprehensive Assessment of CFTR Modulators' Therapeutic Efficiency for N1303K Variant [ Int J Mol Sci, 2024, 25(5)2770]	PubMed: 38474016
Estimation of Chloride Channel Residual Function and Assessment of Targeted Drugs Efficiency in the Presence of a Complex Allele [L467F;F508del] in the CFTR Gene [ Int J Mol Sci, 2024, 25(19)10424]	PubMed: 39408749
PTI-801 (posenacaftor) shares a common mechanism with VX-445 (elexacaftor) to rescue p.Phe508del-CFTR [ Eur J Pharmacol, 2024, 967:176390]	PubMed: 38336013
Localization and function of humanized F508del-CFTR in mouse intestine following activation of serum glucocorticoid kinase 1 and Trikafta [ Eur J Pharmacol, 2024, 978:176771]	PubMed: 38925289
Reduced sialylation of airway mucin impairs mucus transport by altering the biophysical properties of mucin [ Sci Rep, 2024, 14(1):16568]	PubMed: 39019950
Описание клинической картины и оценка функциональной активности канала CFTR у пациента с комплексным аллелем [S466X; R1070Q] [ Pulmonology, 2023, 33 (2): 233–242]	PubMed: None
General trends in the effects of VX-661 and VX-445 on the plasma membrane expression of clinical CFTR variants [ Cell Chem Biol, 2023, S2451-9456(23)00125-3]	PubMed: 37253358
ABC-transporter CFTR folds with high fidelity through a modular, stepwise pathway [ Cell Mol Life Sci, 2023, 80(1):33]	PubMed: 36609925

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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