CFTR corrector 2

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Chemical Structure| 1628416-28-3 同义名 : FDL169
CAS号 : 1628416-28-3
货号 : A1145676
分子式 : C27H23FN4O4
纯度 : 99%
分子量 : 486.494
MDL号 : MFCD32062823
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(123.33 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Cystic fibrosis transmembrane conductance regulator (CFTR), a chloride channel in the membrane of epithelial cells, is essential for salt and fluid homeostasis. Cystic fibrosis is an inherited disorder caused by mutations in the CFTR gene. The most common CFTR mutation (~90%) is the deletion of phenylalanine 508 (F508del). FDL169 is an F508del-CFTR corrector that increases the amount of F508del-CFTR at the cell surface without affecting the open probability of F508del-CFTR. The exposure of cells to FDL169 plus ivacaftor for ≥ 24h led to 15% inhibition. FDL169 had a higher free fraction in human serum than lumacaftor. FDL169 also exhibited improved biodistribution (>4 fold) in mouse lung tissues compared to lumacaftor.[2]
作用机制 FDL169 is a disease-modifying corrector of the F508 deletion that inhibits the folding and stability of the CFTR protein.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.06mL

0.41mL

0.21mL

10.28mL

2.06mL

1.03mL

20.56mL

4.11mL

2.06mL
参考文献

[1]Gross N. The COPD Pipeline XXXII. Chronic Obstr Pulm Dis. 2016 Jul 14;3(3):688-692. doi: 10.15326/jcopdf.3.3.2016.0150

[2]32 Properties of a novel F508del-CFTR corrector FDL169