chemical

7887/10

7887/10

10 mg (also 50 mg)

149 USD

7887/10

Ivacaftor

10 mg (also 50 mg)

Potent and selective CFTR potentiator

CFTR

Small Molecules

98%

392.5

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Ivacaftor is a potent and selective potentiator of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) that targets F508del-CFTR and G551D-CFTR (EC50 values are 25 nM and 100 nM, respectively); its potentiation activity depends on the level of CFTR phosphorylation. Ivacaftor reversibly binds to wild type (WT-CFTR) and G551D-CFTR mutants, increasing the open probability via an ATP-independent mechanism, and enhances cAMP/PKA-signaling mediated gating activity for both WT-CFTR and G551D-CFTR mutants. In cultured human CF bronchial epithelia with G551D/F508del mutations, Ivacaftor increases Forskolin (Cat. No. 1099)-induced transepithelial current (EC50 = 236 nM) and increases chloride secretion by 10-fold. Also rescues endothelial CFTR expression and function and prevents endothelial barrier failure and protein leak in human pulmonary microvascular endothelial cells. Ivacaftor is orally bioavailable.

Potent and selective CFTR potentiator

Potent and selective CFTR potentiator

N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-3-quinolinecarboxamide

C24H28N2O3

C24H28N2O3

873054-44-5

149 USD

Potent and selective CFTR potentiator

ABC35, ABCC7CF, ATP-binding cassette sub-family C member 7, ATP-binding cassette transporter sub-family C member 7, cAMP-dependent chloride channel, CFTR/MRP, Channel conductance-controlling ATPase, cystic fibrosis transmembrane conductance regulator, cystic fibrosis transmembrane conductance regulator (ATP-binding cassettesub-family C, member 7), cystic fibrosis transmembrane conductance regulator, ATP-binding cassette(sub-family C, member 7), dJ760C5.1, EC 3.6.3, MRP7EC 3.6.3.49, TNR-CFTR

Store at -20░C