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

219673
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      주요 사양표

      Empirical FormulaCAS #
      C₂₁H₁₇ClN₄O₂S₂ 421580-53-2

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      219673-10MGCN
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          10 mg
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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 MSDS

          타이틀

          물질안전보건자료(MSDS) 

          CFTR-F508del Corrector II, Corr-4a - CAS 421580-53-2 - Calbiochem Certificates of Analysis

          TitleLot Number
          219673

          References

          참고문헌 보기
          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.
          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.

          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.