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530541 CFTR Potentiator, VX-770 - CAS 873054-44-5 - Calbiochem

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.

CFTR Potentiator, VX-770 - CAS 873054-44-5 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Cystic Fibrosis Transmembrane Conductance Regulator Potentiator, VX 770, Ivacaftor, Kalydeco, N-(5-Hydroxy-2,4-bis(2-methyl-2-propanyl)phenyl]-4-oxo-1,4-dihydro-3-quinolinecarboxamide

Primary Target: WT and G551D mutant forms of cell surface CFTR
530541
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Přehled

Replacement Information

Tabulka spec. kláve

CAS #Empirical Formula
873054-44-5C₂₄H₂₈N₂O₃

Products

Katalogové čísloBalení ks/bal.
5.30541.0001 Skleněná láhev 10 mg
Description
OverviewA 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 µM) 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; EC50 = 236 nM) far more effectively than genistein (EC50 = 16 µM). Displays favorable pharmacokinetic properties with t1/2= 12 h.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number530541
Brand Family Calbiochem®
SynonymsCystic Fibrosis Transmembrane Conductance Regulator Potentiator, VX 770, Ivacaftor, Kalydeco, N-(5-Hydroxy-2,4-bis(2-methyl-2-propanyl)phenyl]-4-oxo-1,4-dihydro-3-quinolinecarboxamide
References
ReferencesNamkung, 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.
Product Information
CAS number873054-44-5
FormOff-white powder
Hill FormulaC₂₄H₂₈N₂O₃
Chemical formulaC₂₄H₂₈N₂O₃
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetWT and G551D mutant forms of cell surface CFTR
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
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 InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Katalogové číslo GTIN
5.30541.0001 04055977260908

Documentation

CFTR Potentiator, VX-770 - CAS 873054-44-5 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Přehled odkazů
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.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision13-June-2014 JSW
SynonymsCystic Fibrosis Transmembrane Conductance Regulator Potentiator, VX 770, Ivacaftor, Kalydeco, N-(5-Hydroxy-2,4-bis(2-methyl-2-propanyl)phenyl]-4-oxo-1,4-dihydro-3-quinolinecarboxamide
DescriptionA 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 µM) 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; EC50 = 236 nM) far more effectively than genistein (EC50 = 16 µM). Displays favorable pharmacokinetic properties with t1/2= 12 h.
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
CAS number873054-44-5
Chemical formulaC₂₄H₂₈N₂O₃
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesNamkung, 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.