Key Documents

View All Documentation

219673-M

CFTR-F508del Corrector II, Corr-4a

Name: CFTR-F508del Corrector II, Corr-4a
Brand: MM

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

Synonym(s):

CFTR-F508del Corrector II, Corr-4a, 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, N-(2-(5-Chloro-2-methoxy-phenylamino)-4ʹ-methyl-[4,5ʹ]bithiazolyl-2ʹ-yl)-benzamide, Corr-4, Cystic Fibrosis Transmembrane Conductor Regulator Mutant Corrector II

Select a Size

Change View

About This Item

Empirical Formula (Hill Notation):

C₂₁H₁₇ClN₄O₂S₂

CAS Number:

421580-53-2

Molecular Weight:

456.97

MDL number:

MFCD02735533

UNSPSC Code:

12352200

NACRES:

NA.32

Assay:

≥95% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, protect from light

Technical Service

Need help? Our team of experienced scientists is here for you.

Let Us Assist

Properties

Quality Level

100

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

light beige

solubility

DMSO: 100 mg/mL

storage temp.

2-8°C

SMILES string

[s]1c(nc(c1c3nc([s]c3)Nc4c(ccc(c4)Cl)OC)C)NC(=O)c2ccccc2

InChI

1S/C21H17ClN4O2S2/c1-12-18(30-21(23-12)26-19(27)13-6-4-3-5-7-13)16-11-29-20(25-16)24-15-10-14(22)8-9-17(15)28-2/h3-11H,1-2H3,(H,24,25)(H,23,26,27)

InChI key

RDOBOPJBMQURAT-UHFFFAOYSA-N

Description

General description

A 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.

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c