219673-M

CFTR-F508del Corrector II, Corr-4a

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

• Synonyme(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
• Formule empirique (notation de Hill): C₂₁H₁₇ClN₄O₂S₂
• Numéro CAS: 421580-53-2
• Poids moléculaire : 456.97
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: light beige
• Solubilité: DMSO: 100 mg/mL
• Température de stockage: 2-8°C
• 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)
• Clé InChI: RDOBOPJBMQURAT-UHFFFAOYSA-N

Description

Description générale

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.

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable