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.

• 同義詞: 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
• 經驗公式（希爾表示法）: C₂₁H₁₇ClN₄O₂S₂
• CAS號碼: 421580-53-2
• 分子量：: 456.97
• MDL號碼: MFCD02735533
• 分類程式碼代碼: 12352200

屬性

• 品質等級: 100
• 化驗: ≥95% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: light beige
• 溶解度: DMSO: 100 mg/mL
• 儲存溫度: 2-8°C
• SMILES 字串: [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 密鑰: RDOBOPJBMQURAT-UHFFFAOYSA-N

描述

一般說明

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.

警告

Toxicity: Standard Handling (A)

重構

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

其他說明

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.

法律資訊

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

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable