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

219673
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Empirical FormulaCAS #
C₂₁H₁₇ClN₄O₂S₂ 421580-53-2

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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®
      SynonymsCystic Fibrosis Transmembrane Conductor Regulator Mutant Corrector II, N-(2-(5-Chloro-2-methoxy-phenylamino)-4ʹ-methyl-[4,5ʹ]bithiazolyl-2ʹ-yl)-benzamide, Corr-4
      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
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      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

      Documentation

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

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      CFTR-F508del Corrector II, Corr-4a - CAS 421580-53-2 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      219673

      Références bibliographiques

      Aperçu de la référence bibliographique
      Pedemonte, 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.
      Fiche technique

      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.

      Revision05-April-2011 RFH
      SynonymsCystic Fibrosis Transmembrane Conductor Regulator Mutant Corrector II, N-(2-(5-Chloro-2-methoxy-phenylamino)-4ʹ-methyl-[4,5ʹ]bithiazolyl-2ʹ-yl)-benzamide, Corr-4
      DescriptionA 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.
      FormLight beige solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number421580-53-2
      Chemical formulaC₂₁H₁₇ClN₄O₂S₂
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage +2°C to +8°C
      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.
      Toxicity Standard Handling
      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.