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Merck - 5.30541.0001 - CFTR Potentiator, VX-770 - CAS 873054-44-5 - Calbiochem

  • MFR SKU: 5.30541.0001
  • ITEM #: 17953634
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ITEM #: 17953634
A cell-permeable, potentiator of CFTR that directly, reversibly, and allosterically binds to WT and G551D mutant forms (~ 10 µM) and increases the open probability to restore lung function.
This listing is for 10 mg Glass bottle

Merck - 5.30541.0001 - CFTR Potentiator, VX-770 - CAS 873054-44-5 - Calbiochem

  • Item #: 17953634
  • MFR SKU: 5.30541.0001
Technical Specs
  • Overview A cell-permeable, orally bioavailable dihydroquinoline-carboxamide compound that acts as a potentiator of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) by directly binding to WT and G551D mutant forms in an allosteric and reversible manner (~ 10 µ M) and increases the open probability to restore lung function. Enhances cAMP/PKA-signaling mediated gating activity of both WT and G551D mutants and its potentiation activity is dependent upon the phosphorylated status of CFTR. Does not compete for binding to the canonical ATP-binding catalytic site; but the rate of flux through CFTR increase by 1.5 to 2 fold when ATP concentrations are increased. Shown to increase Cl - secretion by about 10 fold in cultured human CF bronchial epethelia (HBE) carrying G551D/F508del mutations and increases forskolin-stimulated transepethial current (IT; EC 50 = 236 nM) far more effectively than genistein (EC 50 = 16 µ M). Displays favorable pharmacokinetic properties with t 1/2 = 12 h.
  • Please note that the molecular weight for this compound is batch-specific due to variable water content.
  • Catalogue Number 530541
  • Brand Family Calbiochem®
  • Synonyms N-(5-Hydroxy-2, 4- bis (2-methyl-2-propanyl)phenyl]-4-oxo-1, 4-dihydro-3-quinolinecarboxamide, Cystic Fibrosis Transmembrane Conductance Regulator Potentiator, VX 770, Ivacaftor, Kalydeco
  • References Namkung, W., et al. 2013. Mol. Pharmacol. 84, 384.
  • Eckford, P.D.W., et al. 2012. J. Biol. Chem. 287, 36639.
  • Van Goor, F., et al 2009. Proc. Natl. Acad. Sci. USA 106, 18825.
  • CAS number 873054-44-5
  • Form Off-white powder
  • Hill Formula CHNO
  • Chemical formula CHNO
  • Reversible Y
  • Structure formula Image
  • Quality Level MQ100
  • Primary Target WT and G551D mutant forms of cell surface CFTR
  • Purity ≥ 98% by HPLC
  • Cell permeable Y
  • Ship Code Ambient Temperature Only
  • Toxicity Standard Handling
  • Storage +2° C to +8° C
  • Protect from Light Protect from light
  • Do not freeze Ok to freeze
  • Special Instructions Following reconstitution, aliquot and freeze (-20° C). Stock solutions are stable for up to 6 months at -20° C.
  • Packaged under inert gas Packaged under inert gas
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