2229860-99-3
Chemical Structure
(R)-Elexacaftor
Synonym(s): (R)-VX-445
- CAS No.: 2229860-99-3
- Formula:C26H34F3N7O4S
- Molecular Weight:597.65
IUPAC Name: (R)-N-((1,3-dimethyl-1H-pyrazol-4-yl)sulfonyl)-6-(3-(3,3,3-trifluoro-2,2-dimethylpropoxy)-1H-pyrazol-1-yl)-2-(2,2,4-trimethylpyrrolidin-1-yl)nicotinamide
InChIKey: MVRHVFSOIWFBTE-MRXNPFEDSA-N
SMILES: CC1(C)C[C@@H](C)CN1C2=C(C(NS(C3=CN(C)N=C3C)(=O)=O)=O)C=CC(N4C=CC(OCC(C)(C(F)(F)F)C)=N4)=N2
Biological Activity: (R)-Elexacaftor ((R)-VX-445) is the enantiomer of Elexacaftor (HY-111772). Elexacaftor is an orally active CFTR modulator that targets nucleotide-binding domain 1. Elexacaftor stabilizes misfolded F508del-CFTR protein, enhances its trafficking to the plasma membrane, and significantly improves metabolic stability, thermal stability and ion conductivity. Elexacaftor not only restores chloride transport function in nasal epithelial cells and rescues multiple CFTR mutation subtypes, but also exerts multiplicative synergistic effects with Ivacaftor (HY-13017), and is often used in a triple combination therapy with Tezacaftor (HY-15448). Elexacaftor is widely used in basic and clinical translational research on cystic fibrosis[1][2][3][4][5].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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(R)-Elexacaftor | 99.44% | (R)-Elexacaftor ((R)-VX-445) is the enantiomer of Elexacaftor (HY-111772). Elexacaftor is an orally active CFTR modulator that targets nucleotide-binding domain 1. Elexacaftor stabilizes misfolded F508del-CFTR protein, enhances its trafficking to the plasma membrane, and significantly improves metabolic stability, thermal stability and ion conductivity. Elexacaftor not only restores chloride transport function in nasal epithelial cells and rescues multiple CFTR mutation subtypes, but also exerts multiplicative synergistic effects with Ivacaftor (HY-13017), and is often used in a triple combination therapy with Tezacaftor (HY-15448). Elexacaftor is widely used in basic and clinical translational research on cystic fibrosis. | ||||||||||||||||||||
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- [1]. Carrez T, et al. Effect of elexacaftor and bamocaftor on the metabolic and thermal stability of the F508del-CFTR protein in human airway epithelial cells. Am J Physiol Lung Cell Mol Physiol. 2025;329(5):L583-L597. [Content Brief]
- [2]. Shaughnessy C A, et al. Elexacaftor is a CFTR potentiator and acts synergistically with ivacaftor during acute and chronic treatment[J]. Scientific reports, 2021, 11(1): 19810.
- [3]. Alexander Russell ABELA, et al. Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator. WO2018107100A1. 2017-12-08.
- [4]. Reyne N, et al. Effect of elexacaftor-tezacaftor-ivacaftor on nasal potential difference and lung function in Phe508del rats. Front Pharmacol. 2024;15:1362325. Published 2024 Mar 13. [Content Brief]
- [5]. Sanders M, et al. Evaluation of the drug interaction between rifabutin and elexacaftor/tezacaftor/ivacaftor (ETI). J Cyst Fibros. 2026;25(1):151-157. [Content Brief]
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