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

A cell-permeable bisaminomethylbithiazole compound that is reported to rescue/correct the folding defect of CFTR δF508 mutant via direct interaction.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Cystic Fibrosis Transmembrane Conductor Regulator Mutant Corrector II, N-(2-(5-Chloro-2-methoxy-phenylamino)-4ʹ-methyl-[4,5ʹ]bithiazolyl-2ʹ-yl)-benzamide, Corr-4

219673
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
421580-53-2C₂₁H₁₇ClN₄O₂S₂

Products

Catalogue NumberPackaging Qty/Pack
219673-10MGCN 10 mg
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
Global Trade Item Number
Catalogue Number GTIN
219673-10MGCN 04055977200911

Documentation

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

Title

Safety Data Sheet (SDS) 

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

TitleLot Number
219673

References

Reference overview
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 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
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.