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 (1 µM Lumacaftor +0.02 µM Ivacaftor +3 µM Elexacaftor) 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 (1 µM Lumacaftor +0.02 µM Ivacaftor +3 µM Elexacaftor) 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 52 publications

PTI-801 (posenacaftor) shares a common mechanism with VX-445 (elexacaftor) to rescue p.Phe508del-CFTR [ Eur J Pharmacol, 2024, 967:176390]	PubMed: 38336013
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
A Novel Co-Culture Model Reveals Enhanced CFTR Rescue in Primary Cystic Fibrosis Airway Epithelial Cultures with Persistent Pseudomonas aeruginosa Infection [ Cells, 2023, 10.3390/cells12222618]	PubMed: 37998353
UBE3C Facilitates the ER-Associated and Peripheral Degradation of Misfolded CFTR [ Cells, 2023, 12(23)2741]	PubMed: 38067172
Elexacaftor Mediates the Rescue of F508del CFTR Functional Expression Interacting with MSD2 [ Int J Mol Sci, 2023, 10.3390/ijms241612838]	PubMed: 37629017
Putting bicarbonate on the spot: pharmacological insights for CFTR correction in the airway epithelium [ Front Pharmacol, 2023, 14:1293578]	PubMed: 38149052
The COPD-Associated Polymorphism Impairs the CFTR Function to Suppress Excessive IL-8 Production upon Environmental Pathogen Exposure [ Int J Mol Sci, 2023, 24(3)2305]	PubMed: 36768629
Elexacaftor Mediates the Rescue of F508del CFTR Functional Expression Interacting with MSD2 [ Int J Mol Sci, 2023, 24(16)12838]	PubMed: 37629017
TGF-β1 inhibition of ACE2 mediated by miRNA uncovers novel mechanism of SARS-CoV-2 pathogenesis [ J Innate Immun, 2023, 15(1):629-46]	PubMed: 37579743

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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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