CFTR corrector 2是囊性纤维化跨膜电导调节因子 (CFTR) 的调节剂,CFTR 是一种位于上皮细胞膜上的氯离子通道,对盐和液体的稳态至关重要。
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产品名称 | CFTR ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Ataluren | ✔ | 98% | |||||||||||||||||
Lumacaftor |
++++
F508del-CFTR, EC50: 0.1 μM |
98% | |||||||||||||||||
CFTR(inh)-172 |
+++
CFTR, Ki: 300 nM |
99%+ | |||||||||||||||||
GlyH-101 |
+
CFTR, Ki: 4.3 μM |
99%+ | |||||||||||||||||
IOWH-032 |
++
CFTR, IC50: 1.01 μM |
99%+ | |||||||||||||||||
Tezacaftor | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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] |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 1628416-28-3 |
分子式 | C27H23FN4O4 |
分子量 | 486.494 |
别名 | FDL169 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
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 |