| Identification | Back Directory | [Name]
N-(2-[(5-CHLORO-2-METHOXYPHENYL)AMINO]-4'-METHYL-4,5'-BI-1,3-THIAZOL-2'-YL)BENZAMIDE | [CAS]
421580-53-2 | [Synonyms]
Corrector C4
N-[5-[2-(5-Chloro-2-methoxy-anilino)thiazol-4-yl]-4-methyl-thiazol-2-yl]benzamide
N-[2-(5-CHLORO-2-METHOXY-PHENYLAMINO)-4'-METHYL-[4,5']BITHIAZOLYL-2'-YL]-BENZAMIDE
Benzamide, N-[2-[(5-chloro-2-methoxyphenyl)amino]-4'-methyl[4,5'-bithiazol]-2'-yl]-
N-(2-[(5-CHLORO-2-METHOXYPHENYL)AMINO]-4'-METHYL-4,5'-BI-1,3-THIAZOL-2'-YL)BENZAMIDE
N-(2-[(5-CHLORO-2-METHOXYPHENYL)AMINO]-4'-METHYL-4,5'-BI-1,3-THIAZOL-2'-YL)BENZAMIDE
N-[5-[2-(5-chloro-2-methoxyanilino)-1,3-thiazol-4-yl]-4-methyl-1,3-thiazol-2-yl]benzamide | [Molecular Formula]
C21H17ClN4O2S2 | [MDL Number]
MFCD02735533 | [MOL File]
421580-53-2.mol | [Molecular Weight]
456.97 |
| Chemical Properties | Back Directory | [density ]
1.440±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 100mg/mL | [form ]
solid | [pka]
6.81±0.70(Predicted) | [color ]
light beige |
| Hazard Information | Back Directory | [Uses]
Corr4A is a chemical corrector, which can be used for cystic fibrosis. Corr4A interacts directly with the cystic fibrosis transmembrane conductance regulator (CFTR) or affects indirectly its folding process. Corr4A increases the expression of CFTR ΔF508 on the cell surface, thereby improving its transport to the plasma membrane and increasing the stability of the rescued mutant protein[1]. | [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. | [References]
[1] Grove DE, et al., Mechanisms for rescue of correctable folding defects in CFTRDelta F508. Mol Biol Cell. 2009 Sep;20(18):4059-69. DOI:10.1091/mbc.e08-09-0929 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
| Company Name: |
Biorbyt Ltd.
|
| Tel: |
+44 (0)1223 859 353 |
| Website: |
http://www.biorbyt.com |
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