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219673 CFTR-F508del Corrector II, Corr-4a - CAS 421580-53-2 - Calbiochem

Descripción

Tabla espec. clave

CAS #Empirical Formula
421580-53-2C₂₁H₁₇ClN₄O₂S₂

Precios y disponibilidad

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219673-10MG
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      Description
      OverviewA cell-permeable bisaminomethylbithiazole compound that is reported to rescue/correct the folding defect of CFTR ΔF508 mutant via direct interaction and promote proper trafficking/glycosylation and surface expression in both transfected cells and primary airway epithelial cells from ΔF508-homozygous patients, while exhibiting little correcting effect toward N1303K-CFTR, P574H-CFTR, M345T-DRD4 (dopamine receptor 4), or G268V-ABCA1/CD243 /MDR1/ P-gp mutant. Reported to enhance the folding efficiency of both ΔF508 (by 3-fold at 10µM in FRT cells) and wild-type CFTR (by up to 70%), delay the ER-associated degradation of the core-glycosylated ΔF508 (by 30% at 10µM in FRT cells), and increase the stability of low-temperature resuced ΔF508 mutant on the plasma membrane (by 1.7-fold at 10µM in FRT cells). Corr-4a is shown to be more effective than VRT-325/CFcor-325 n restoring forskolin-stimulated CFTR activity in FRT and A549 ΔF508-CFTR transfectants. Unlike VRT-532 Corr-4a does not affect mutant CFTR channel gating activity.
      Catalogue Number219673
      Brand Family Calbiochem®
      SynonymsN-(2-(5-Chloro-2-methoxy-phenylamino)-4ʹ-methyl-[4,5ʹ]bithiazolyl-2ʹ-yl)-benzamide, Corr-4, Cystic Fibrosis Transmembrane Conductor Regulator Mutant Corrector II
      References
      ReferencesPedemonte, N., et al. 2010. Am. J. Physiol. Cell Physiol. 298, C866.
      Young, A., et al. 2009. Biochem. J. 421, 377.
      Wang, Y., et al. 2007. J. Biol. Chem. 282, 33247.
      Wang, Y., et al. 2007. Mol. Pharmacol. 71, 751.
      Wang, Y., et al. 2007. Biochem. J. 406, 257.
      Pedemonte, N., et al. 2005. J. Clin. Invest. 115, 2564.
      Product Information
      CAS number421580-53-2
      FormLight beige solid
      Hill FormulaC₂₁H₁₇ClN₄O₂S₂
      Chemical formulaC₂₁H₁₇ClN₄O₂S₂
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Purity≥95% by HPLC
      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
      Global Trade Item Number
      Número de referencia GTIN
      219673-10MG 04055977200911