Elexacaftor

SKU: orb1308463

Description

Elexacaftor

Research Area

Cell Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2216712-66-0
• MW: 597.65
• Purity: 98.87% (May vary between batches)
• Formula: C₂₆H₃₄F₃N₇O₄S
• SMILES: C(NS(=O)(=O)C1=CN(C)N=C1C)(=O)C2=C(N=C(C=C2)N3N=C(OCC(C(F)(F)F)(C)C)C=C3)N4C[C@@H](C)CC4(C)C
• Target: Autophagy,CFTR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (6.69 mM);DMSO:125 mg/mL (209.15 mM)

Bioactivity

• Target IC50:
  CFTR:1.01 μM
• In Vivo:
  METHODS: Patients with the Phe508del–Phe508del genotype underwent a 4-week run-in of tezacaftor and ivacaftor and were randomized to receive either elexacaftor (VX-445) (200 mg orally daily) plus tezacaftor (100 mg daily) and ivacaftor (150 mg daily) or matching placebo plus tezacaftor and ivacaftor for 4 weeks. RESULTS Treatment with elexacaftor (VX-445)-tezacaftor-ivacaftor significantly increased the percentage predicted FEV1 by up to 13.8 percentage points in patients with the Phe508del-MF genotype and up to 11.0 percentage points in patients with the Phe508del-Phe508del genotype who were already receiving tezacaftor-ivacaftor.
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• In Vitro:
  Elexacaftor (VX-445) has the potential to treat cystic fibrosis and it also is a next-generation cystic fibrosis transmembrane conductance regulator (CFTR) corrector designed to restore Phe508del CFTR protein function. VX-445-Tezacaftor-VX-770 significantly improves Phe508del CFTR protein processing, trafficking, chloride transport. To a greater extent than any two of these agents in dual combination.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, Cystic, Cystic fibrosis transmembrane conductance regulator, CFTR, inhibit, Inhibitor, Fibrosis, Elexacaftor, VX 445, VX445, VX-445

Compound Identifiers

PubChem CID

134587348