Chemical Structure : Posenacaftor
CAS No.:
2095064-05-2
Posenacaftor
(PTI-801, PTI 801)
Catalog No.: PC-22022Not For Human Use, Lab Use Only.
Posenacaftor (PTI-801) is a newly developed p.Phe508del-CFTR corrector with EC50 of 0.52 uM (HS-YFP quenching rate).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Posenacaftor (PTI-801) is a newly developed p.Phe508del-CFTR corrector with EC50 of 0.52 uM (HS-YFP quenching rate).
Posenacaftor (PTI-801) at 1 and 3 μM concentrations also demonstrated greater efficacy in rescuing p.Phe508del-CFTR function than VX-661 at 5 μM concentration.
Posenacaftor (PTI-801) rescues p.Phe508del-CFTR processing, PM trafficking, and channel function (upon agonist stimulation) with greater correction effects in combination with ABBV-2222, FDL-169, VX-661, or VX-809, but not with VX-445.
Posenacaftor (PTI-801) exhibits no potentiator activity on low temperature- and corrector-rescued p.Phe508del-CFTR, displays similar behavior to that of VX-445 on genetic revertants.
Physicochemical Properties
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M.Wt
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445.52
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Formula
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C27H27NO5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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8-Methyl-2-(3-methyl-2-benzofuranyl)-5-[(1R)-1-(tetrahydro-2H-pyran-4-yl)ethoxy]-4-quinolinecarboxylic acid
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References
1. Filipa C Ferreira, et al. Eur J Pharmacol. 2024 Mar 15:967:176390.
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