Elexacaftor (VX-445)

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

Elexacaftor (VX-445) Chemical Structure

Elexacaftor (VX-445) Chemical Structure

CAS: 2216712-66-0

Selleck's Elexacaftor (VX-445) has been cited by 50 publications

Purity & Quality Control

Batch: S885101 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.67%
99.67

Choose Selective CFTR Inhibitors

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
In vitro

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

Cell Research 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)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05519020 Recruiting Cystic Fibrosis Sheffield Teaching Hospitals NHS Foundation Trust July 27 2022 --
NCT03525548 Completed Cystic Fibrosis Vertex Pharmaceuticals Incorporated August 3 2018 Phase 3
NCT03525444 Completed Cystic Fibrosis Vertex Pharmaceuticals Incorporated June 15 2018 Phase 3

Chemical lnformation & Solubility

Molecular Weight 597.65 Formula

C26H34F3N7O4S

CAS No. 2216712-66-0 SDF --
Smiles CC1CC(N(C1)C2=C(C=CC(=N2)N3C=CC(=N3)OCC(C)(C)C(F)(F)F)C(=O)NS(=O)(=O)C4=CN(N=C4C)C)(C)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (167.32 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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