Molecular structure of Ivacaftor, CAS Number: 873054-44-5
Ivacaftor (CAS 873054-44-5)
Alternate Names:
VX-770
Application:
Ivacaftor is is a CFTR activator
CAS Number:
873054-44-5
Purity:
≥98%
Molecular Weight:
392.49
Molecular Formula:
C24H28N2O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Ivacaftor is a CFTR activator (IC50 of 43 ± 38 nM). In some cells Ivacaftor was shown to increase CFTR channel open probability in the F508del processing and the G551D gating mutations. In cultured human CF bronchial epithelia (HBE) expressing the F551D gating mutation on one allele and F508del processing mutation on the other allele, Ivacaftor was shown to increase Cl- secretion by about 10-fold, to about 50% of that observed in HBE isolated from individuals without CF, in addition, Ivacaftor reduced excessive Na+ and fluid absorption preventing dehydration of the apical surface and increased cilia beating in these epithelial cultures.
Ivacaftor (CAS 873054-44-5) References
- Synthetic aminoglycosides efficiently suppress cystic fibrosis transmembrane conductance regulator nonsense mutations and are enhanced by ivacaftor. | Xue, X., et al. 2014. Am J Respir Cell Mol Biol. 50: 805-16. PMID: 24251786
- Discovery of N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide (VX-770, ivacaftor), a potent and orally bioavailable CFTR potentiator. | Hadida, S., et al. 2014. J Med Chem. 57: 9776-95. PMID: 25441013
- Potentiators of Defective ΔF508-CFTR Gating that Do Not Interfere with Corrector Action. | Phuan, PW., et al. 2015. Mol Pharmacol. 88: 791-9. PMID: 26245207
- Discovery of Clinically Approved Agents That Promote Suppression of Cystic Fibrosis Transmembrane Conductance Regulator Nonsense Mutations. | Mutyam, V., et al. 2016. Am J Respir Crit Care Med. 194: 1092-1103. PMID: 27104944
- Fatty Acid Cysteamine Conjugates as Novel and Potent Autophagy Activators That Enhance the Correction of Misfolded F508del-Cystic Fibrosis Transmembrane Conductance Regulator (CFTR). | Vu, CB., et al. 2017. J Med Chem. 60: 458-473. PMID: 27976892
- Residual function of cystic fibrosis mutants predicts response to small molecule CFTR modulators. | Han, ST., et al. 2018. JCI Insight. 3: PMID: 30046002
- Inhalable nano into micro dry powders for ivacaftor delivery: The role of mannitol and cysteamine as mucus-active agents. | Porsio, B., et al. 2020. Int J Pharm. 582: 119304. PMID: 32272167
- Ivacaftor Reverses Airway Mucus Abnormalities in a Rat Model Harboring a Humanized G551D-CFTR. | Birket, SE., et al. 2020. Am J Respir Crit Care Med. 202: 1271-1282. PMID: 32584141
- Ivacaftor partially corrects airway inflammation in a humanized G551D rat. | Green, M., et al. 2021. Am J Physiol Lung Cell Mol Physiol. 320: L1093-L1100. PMID: 33825507
- Entry of cystic fibrosis transmembrane conductance potentiator ivacaftor into the developing brain and lung. | Qiu, F., et al. 2021. J Cyst Fibros. 20: 857-864. PMID: 34193363
- Muc5b Contributes to Mucus Abnormality in Rat Models of Cystic Fibrosis. | Keith, JD., et al. 2022. Front Physiol. 13: 884166. PMID: 35574458
- Ivacaftor Alters Macrophage and Lymphocyte Infiltration in the Lungs Following Lipopolysaccharide Exposure. | Harwood, KH., et al. 2022. ACS Pharmacol Transl Sci. 5: 419-428. PMID: 35711814
- Congenital bilateral cataracts in newborns exposed to elexacaftor-tezacaftor-ivacaftor in utero and while breast feeding. | Jain, R., et al. 2022. J Cyst Fibros. 21: 1074-1076. PMID: 36266182
- Elexacaftor/Tezacaftor/Ivacaftor Disrupts Respiratory Tract Development in a Murine Fetal Lung Explant Model. | Lhuillier, M., et al. 2022. Am J Respir Cell Mol Biol. 67: 723-726. PMID: 36454086
- Developmental changes in the extent of drug binding to rat plasma proteins. | Qiu, F., et al. 2023. Sci Rep. 13: 1266. PMID: 36690711
Inhibitor of:
CFTR.Activator of:
CFTR.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Ivacaftor, 5 mg | sc-364679 | 5 mg | $259.00 |